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(5'-GATCTAAAAGACTT-3')-phosphotyrosine + H2O
(5'-GATCTAAAAGACTT-3')-phosphate + L-tyrosine
-
-
-
?
10-hydroxydecyl-oligonucleotide + H2O
?
-
different sequences of the oligonucleotides, overview. The enzyme catalyzes the cleavage of the synthetic analogue of the apurinic/apyrimidinic site
-
-
?
2',3'-cAMP + H2O
?
-
-
-
-
?
2-hydroxypropyl-p-nitrophenyl phosphate + H2O
2-hydroxypropyl-p-nitrophenol + phosphate
-
-
-
?
2-naphthyl chloromethylphosphonate + H2O
2-naphthol + chloromethylphosphonic acid
-
-
-
-
?
2-naphthyl methylphosphonate + H2O
2-naphthol + methylphosphonic acid
-
-
-
-
?
2-naphthyl phenylphosphonate + H2O
2-naphthol + benzenephosphonic acid
-
-
-
-
?
3'-O-acetyl-5'-O-[hydroxy(4-nitrophenoxy)phosphoryl]thymidine + H2O
p-nitrophenol + 3'-O-acetylthymidine 5'-phosphate
-
-
-
-
?
3'-p-nitrophenylthymidine 3'-phosphate + H2O
3'-TMP + p-nitrophenol
-
-
-
-
?
3'-phosphoadenosine 5'-phosphosulfate + H2O
?
-
-
-
-
?
3'-phosphohistidyl-linked tyrosyl-DNA phosphodiesterase I-DNA complex + H2O
?
tyrosyl-DNA phosphodiesterase I hydrolyzes the 3'phospho-histidyl bond formed between tyrosyl-DNA phosphodiesterase I and DNA
-
-
?
3'-phosphotyrosyl-linked topoisomerase I-DNA complex + H2O
?
tyrosyl-DNA phosphodiesterase I hydrolyzes the 3'phospho-tyrosyl bond formed between DNA topoisomerase I and DNA
-
-
?
3-hydroxy-2(hydroxymethyl)-tetrahydrofuran-oligonucleotide + H2O
?
-
different sequences of the oligonucleotides, overview. The enzyme catalyzes the cleavage of the synthetic analogue of the apurinic/apyrimidinic site. In the case of tetrahydrofuran, the enzyme generates break with the 5'-tetrahydrofuran and the 3'-phosphate termini
the enzyme generates a non-phosphorylated 5'-THF-terminus by the cleavage of 3-hydroxy-2(hydroxymethyl)-tetrahydrofuran-containing DNA
-
?
4-methylumbelliferyl phenylphosphonate + H2O
4-methylumbelliferone + phenylphosphonic acid
-
-
-
-
?
4-methylumbelliferyl thymidine 5'-phosphate + H2O
4-methylumbelliferone + 5'-TMP
-
-
-
-
?
4-nitrophenyl deoxythymidine 5'-phosphate + H2O
4-nitrophenol + deoxythymidine 5'-phosphate
-
-
-
-
?
4-nitrophenyl phenyl phosphonate + H2O
4-nitrophenol + phenyl phosphonate
-
-
-
-
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
-
-
-
-
?
4-nitrophenyl phosphocholine + H2O
4-nitrophenol + phosphocholine
secreted recombinant human SMPDL3A hydrolyzes 4-nitrophenyl phosphorylcholine, a synthetic analogue of the phosphorylcholine headgroup of lipids such as sphingomyelin and phosphatidylcholine
-
-
?
4-nitrophenyl phosphorothioate + H2O
?
-
-
-
-
?
4-nitrophenyl sulfate + H2O
?
-
-
-
-
?
4-nitrophenyl uridine 5'-phosphate + H2O
4-nitrophenol + uridine 5'-phosphate
5'-(5,6-FAM-aacgtcagggtcttcc-BHQ1)-3' + H2O
?
5'-p-nitrophenyl deoxythymidine 5'-phosphate + H2O
5'-dTMP + p-nitrophenol
5'-p-nitrophenyl-2',3'-isopropyl-5'-UMP + H2O
?
-
-
-
-
?
5'-p-nitrophenyladenosine 5'-phosphate + H2O
5'-AMP + p-nitrophenol
-
FS-44: bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase
-
-
?
5'-p-nitrophenylnucleoside 5'-monophosphate + H2O
nucleoside 5'-monophosphate + p-nitrophenol
5'-p-nitrophenyluridine 5'-phosphate + H2O
5'-UMP + p-nitrophenol
5'-phosphotyrosyl-linked topoisomerase II-DNA complex + H2O
?
tyrosyl-DNA phosphodiesterase I hydrolyzes the 5'phospho-tyrosyl bond formed between DNA topoisomerase II and DNA
-
-
?
adenosine 5'-P1-tetraphospho-P4-5'''-adenosine + H2O
AMP + ATP
adenosine 5'-P1-tetraphospho-P4-5'''-guanosine + H2O
?
-
-
-
-
?
adenosine 5'-phosphosulfate + H2O
?
-
-
-
-
?
adenylyl-2',5'-adenosine + H2O
?
-
FS-44: bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase
-
-
?
adenylyl-3',5'-adenosine + H2O
adenosine + 5'-AMP
adenylyl-3',5'-cytidine + H2O
adenosine 3'-phosphate + cytidine
-
FS-44: bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase
-
-
?
adenylyl-3',5'-uridine + H2O
5'-UMP + adenosine
-
-
-
?
adenylyl-3',5'-uridine + H2O
?
-
FS-44: bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase
-
-
?
ADP + H2O
AMP + phosphate
ADP-ribose + H2O
5'-AMP + ribosyl monophosphate
-
-
-
?
ADP-ribose + H2O
?
-
-
-
?
ApA + H2O
5'-AMP + adenosine
ApC + H2O
5'-CMP + adenosine
-
-
-
?
ApG + H2O
5'-GMP + adenosine
-
-
-
?
ATP + H2O
5'-AMP + diphosphate
ATP + H2O
AMP + diphosphate
-
-
-
-
?
bis(4-methylumbelliferyl) phosphate + H2O
?
-
-
-
-
?
bis(4-nitrophenyl) phosphate + H2O
4-nitrophenyl phosphate + 4-nitrophenol
-
-
-
-
?
bis(4-nitrophenyl)phosphate + H2O
4-nitrophenyl phosphate + 4-nitrophenol
-
-
-
-
?
bis(p-nitrophenyl) phosphate + H2O
?
bis-4-nitrophenyl phosphate + H2O
4-nitrophenol + 4-nitrophenyl phosphate
-
-
-
-
?
bis-ethylene glycolyl-oligonucleotide + H2O
?
-
different sequences of the oligonucleotides, overview. The enzyme catalyzes the cleavage of the synthetic analogue of the apurinic/apyrimidinic site
-
-
?
bis-p-nitrophenyl phosphate + H2O
p-nitrophenol + p-nitrophenyl phosphate
bis-p-nitrophenyl phosphate + H2O
p-nitrophenyl phosphate + nitrophenol
CDP-choline + H2O
?
-
-
-
-
?
CpU + H2O
5'-UMP + cytidine
-
-
-
?
cyclic 3',5'-mononucleotides + H2O
mononucleoside 5'-phosphate
cytidylyl-3',5'-adenosine + H2O
?
-
FS-44: bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase
-
-
?
diadenosine 5',5'''-P1,P3-triphosphate + H2O
AMP + ADP
diadenosine diphosphate + H2O
?
-
-
-
-
?
diadenosine polyphosphate + H2O
AMP + adenosine polyphosphate-1
diethenoadenosine polyphosphate + H2O
ethenoadenosine 5'-monophosphate + ethenoadenosine (n-1)5'-polyphosphate
-
-
-
-
?
diguanosine 5',5'''-P1,P4-tetraphosphate + H2O
?
-
-
-
-
?
dinucleoside monophosphates + H2O
mononucleoside 5'-phosphate
dinucleoside polyphosphate + H2O
?
dinucleoside tetraphosphate + H2O
?
-
-
-
-
?
DNA + H2O
DNA(n-1) + 2'-deoxynucleoside 5'-phosphate
downstream cleavage product-RNA + H2O
?
-
-
-
-
?
FAD + H2O
AMP + FMN
-
-
-
?
GDP-mannose + H2O
?
-
-
-
-
?
guanylyl-3',5'-adenosine + H2O
?
-
FS-44: bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase
-
-
?
methyl 4-nitrophenyl phosphorothioate + H2O
?
-
-
-
-
?
NADP+ + H2O
NAD+ + phosphate
oligonucleotides + H2O
oligonucleotides(n-1) + 5'-mononucleotides
p-nitrophenyl 5'-thymidine monophosphate + H2O
5'-TMP + p-nitrophenol
-
-
-
?
p-nitrophenyl 5'-thymidine monophosphate + H2O
p-nitrophenol + 5'-thymidine monophosphate
p-nitrophenyl chloromethylphosphonate + H2O
p-nitrophenol + chloromethylphosphonic acid
-
-
-
-
?
p-nitrophenyl ethyl phosphate + H2O
p-nitrophenol + ethyl hydrogen phosphate
-
-
-
-
?
p-nitrophenyl methylphosphonate + H2O
p-nitrophenol + methylphosphonic acid
-
-
-
-
?
p-nitrophenyl phenylphosphonate + H2O
p-nitrophenol + benzenephosphonic acid
p-nitrophenyl phenylphosphonate + H2O
p-nitrophenol + phenylphosphonic acid
-
-
-
-
?
p-nitrophenylphosphorylcholine + H2O
p-nitrophenol + phosphorylcholine
p-nitrophenylthymidine 5'-phosphate + H2O
5'-TMP + p-nitrophenol
P1,P4-bis(5'-uridyl) tetraphosphate + H2O
UMP + uridine 5'-triphosphate
-
-
-
?
phosphonate ester + H2O
?
-
-
-
-
?
poly d(A-T)2 + H2O
?
-
-
-
-
?
poly G + H2O
5'-GMP
-
-
-
?
polymer synthesized from NAD+ + H2O
?
-
chain length 27-30
-
-
?
polynucleotides + H2O
polynucleotides(n-1) + 5'-mononucleotides
RNA + H2O
5'-GMP + 5'-AMP + ?
-
-
-
?
RNA + H2O
RNA(n-1) + nucleoside 5'-phosphate
thymidine 5'-monophosphate p-nitrophenylester + H2O
? + phosphate
-
-
-
?
thymidine 5'-monophosphate p-nitrophenylester + H2O
p-nitrophenol + TMP
-
-
-
?
thymidine 5'-triphosphate + H2O
?
-
-
-
-
?
TpT + H2O + H2O
5'-TMP + thymidine
-
calf
-
?
UDP-glucose + H2O
glucose-1-phosphate + 5'-UMP
uridylyl-3',5'-adenosine + H2O
?
-
FS-44: bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase
-
-
?
UTP + H2O
UMP + diphosphate
-
-
-
?
additional information
?
-
4-nitrophenyl uridine 5'-phosphate + H2O
4-nitrophenol + uridine 5'-phosphate
-
-
-
-
?
4-nitrophenyl uridine 5'-phosphate + H2O
4-nitrophenol + uridine 5'-phosphate
-
-
-
-
?
5'-(5,6-FAM-aacgtcagggtcttcc-BHQ1)-3' + H2O
?
-
-
-
?
5'-(5,6-FAM-aacgtcagggtcttcc-BHQ1)-3' + H2O
?
-
-
-
?
5'-p-nitrophenyl deoxythymidine 5'-phosphate + H2O
5'-dTMP + p-nitrophenol
-
-
-
-
?
5'-p-nitrophenyl deoxythymidine 5'-phosphate + H2O
5'-dTMP + p-nitrophenol
-
-
-
-
?
5'-p-nitrophenyl deoxythymidine 5'-phosphate + H2O
5'-dTMP + p-nitrophenol
-
-
-
-
?
5'-p-nitrophenyl deoxythymidine 5'-phosphate + H2O
5'-dTMP + p-nitrophenol
-
nucleotide pyrophosphatase/phosphodiesterase I
-
-
?
5'-p-nitrophenylnucleoside 5'-monophosphate + H2O
nucleoside 5'-monophosphate + p-nitrophenol
-
-
-
?
5'-p-nitrophenylnucleoside 5'-monophosphate + H2O
nucleoside 5'-monophosphate + p-nitrophenol
-
-
-
-
?
5'-p-nitrophenylnucleoside 5'-monophosphate + H2O
nucleoside 5'-monophosphate + p-nitrophenol
-
-
-
-
?
5'-p-nitrophenylnucleoside 5'-monophosphate + H2O
nucleoside 5'-monophosphate + p-nitrophenol
-
-
-
?
5'-p-nitrophenyluridine 5'-phosphate + H2O
5'-UMP + p-nitrophenol
-
-
-
-
?
5'-p-nitrophenyluridine 5'-phosphate + H2O
5'-UMP + p-nitrophenol
-
70% as fast as 5'-p-nitrophenylthymidine 5'-phosphate
-
-
?
adenosine 5'-P1-tetraphospho-P4-5'''-adenosine + H2O
AMP + ATP
-
-
-
?
adenosine 5'-P1-tetraphospho-P4-5'''-adenosine + H2O
AMP + ATP
-
-
-
?
adenosine 5'-P1-tetraphospho-P4-5'''-adenosine + H2O
AMP + ATP
-
-
-
-
?
adenosine 5'-P1-tetraphospho-P4-5'''-adenosine + H2O
AMP + ATP
-
-
-
-
?
adenylyl-3',5'-adenosine + H2O
adenosine + 5'-AMP
-
FS-44: bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase
-
-
?
adenylyl-3',5'-adenosine + H2O
adenosine + 5'-AMP
-
-
-
?
ADP + H2O
AMP + phosphate
-
-
-
-
?
ADP + H2O
AMP + phosphate
-
-
-
?
ADP + H2O
AMP + phosphate
-
slowly
-
-
?
ADP + H2O
AMP + phosphate
-
pyrophosphatase activity
-
-
?
ADP + H2O
AMP + phosphate
-
-
-
?
ADP + H2O
AMP + phosphate
-
PC-1
-
-
?
ADP + H2O
AMP + phosphate
-
ADPase activity, hydrolysis of ADP by human plasma PDEase acts as an inhibitor of platelet aggregation
-
?
ADP + H2O
AMP + phosphate
-
-
-
-
?
ADP + H2O
AMP + phosphate
-
PC-1
-
-
?
ADP + H2O
AMP + phosphate
-
-
-
-
?
ADP + H2O
AMP + phosphate
-
-
-
-
?
ADP + H2O
AMP + phosphate
-
slowly
-
-
?
ApA + H2O
5'-AMP + adenosine
-
-
-
-
?
ApA + H2O
5'-AMP + adenosine
-
-
-
?
ATP + H2O
5'-AMP + diphosphate
-
-
-
?
ATP + H2O
5'-AMP + diphosphate
-
slowly
-
-
?
ATP + H2O
5'-AMP + diphosphate
-
calf
-
?
ATP + H2O
5'-AMP + diphosphate
-
pyrophosphatase activity
-
-
?
ATP + H2O
5'-AMP + diphosphate
-
-
-
?
ATP + H2O
5'-AMP + diphosphate
-
-
-
-
?
ATP + H2O
5'-AMP + diphosphate
-
PC-1
-
-
?
ATP + H2O
5'-AMP + diphosphate
-
-
-
-
?
ATP + H2O
5'-AMP + diphosphate
-
PC-1
-
-
?
ATP + H2O
5'-AMP + diphosphate
-
-
-
-
?
ATP + H2O
5'-AMP + diphosphate
-
-
-
-
?
ATP + H2O
5'-AMP + diphosphate
-
PC-1
PC-1
?
ATP + H2O
5'-AMP + diphosphate
-
-
-
-
?
ATP + H2O
5'-AMP + diphosphate
-
slowly
-
-
?
ATP + H2O
5'-AMP + diphosphate
-
-
-
-
?
bis(p-nitrophenyl) phosphate + H2O
?
-
-
-
-
?
bis(p-nitrophenyl) phosphate + H2O
?
-
-
-
-
?
bis(p-nitrophenyl) phosphate + H2O
?
-
-
-
-
?
bis(p-nitrophenyl) phosphate + H2O
?
-
-
-
-
?
bis(p-nitrophenyl) phosphate + H2O
?
-
-
-
-
?
bis(p-nitrophenyl) phosphate + H2O
?
-
-
-
-
?
bis(p-nitrophenyl) phosphate + H2O
?
-
-
-
-
?
bis(p-nitrophenyl) phosphate + H2O
?
-
-
-
-
?
bis-p-nitrophenyl phosphate + H2O
p-nitrophenol + p-nitrophenyl phosphate
-
-
processive two-step mechanism
-
?
bis-p-nitrophenyl phosphate + H2O
p-nitrophenol + p-nitrophenyl phosphate
-
-
-
?
bis-p-nitrophenyl phosphate + H2O
p-nitrophenol + p-nitrophenyl phosphate
-
-
-
?
bis-p-nitrophenyl phosphate + H2O
p-nitrophenol + p-nitrophenyl phosphate
-
-
-
?
bis-p-nitrophenyl phosphate + H2O
p-nitrophenyl phosphate + nitrophenol
-
-
-
-
?
bis-p-nitrophenyl phosphate + H2O
p-nitrophenyl phosphate + nitrophenol
-
-
-
-
?
cAMP + H2O
?
-
-
-
-
?
cAMP + H2O
?
-
incubated with or without 0.2 mM CaCl2, 10 mU calmodulin, and PDE1 inhibitor vinpocetin, 30°C, pH 7.5
-
-
?
cyclic 3',5'-mononucleotides + H2O
mononucleoside 5'-phosphate
-
3',5'-cAMP, slowly
-
-
?
cyclic 3',5'-mononucleotides + H2O
mononucleoside 5'-phosphate
-
PDE1 inhibitory activity assays
-
-
?
cyclic 3',5'-mononucleotides + H2O
mononucleoside 5'-phosphate
-
cyclic AMP: not a substrate
-
-
?
cyclic 3',5'-mononucleotides + H2O
mononucleoside 5'-phosphate
-
PC-1
-
-
?
cyclic 3',5'-mononucleotides + H2O
mononucleoside 5'-phosphate
-
phosphodiester bonds
-
?
cyclic 3',5'-mononucleotides + H2O
mononucleoside 5'-phosphate
-
phosphodiester bonds
-
-
?
cyclic 3',5'-mononucleotides + H2O
mononucleoside 5'-phosphate
-
PC-1
-
-
?
cyclic 3',5'-mononucleotides + H2O
mononucleoside 5'-phosphate
-
phosphodiester bonds
-
-
?
cyclic 3',5'-mononucleotides + H2O
mononucleoside 5'-phosphate
-
slowly
-
?
diadenosine 5',5'''-P1,P3-triphosphate + H2O
AMP + ADP
-
-
-
?
diadenosine 5',5'''-P1,P3-triphosphate + H2O
AMP + ADP
-
-
-
?
diadenosine 5',5'''-P1,P3-triphosphate + H2O
AMP + ADP
-
-
-
-
?
diadenosine polyphosphate + H2O
AMP + adenosine polyphosphate-1
-
-
-
?
diadenosine polyphosphate + H2O
AMP + adenosine polyphosphate-1
-
phosphodiesterase can be considered as a catabolic enzyme
-
-
?
diadenosine polyphosphate + H2O
AMP + adenosine polyphosphate-1
-
phosphodiesterase can be considered as a catabolic enzyme
-
?
dinucleoside monophosphates + H2O
mononucleoside 5'-phosphate
-
-
-
?
dinucleoside monophosphates + H2O
mononucleoside 5'-phosphate
-
3'-5' linkage
-
-
?
dinucleoside monophosphates + H2O
mononucleoside 5'-phosphate
-
no specificity toward bases or sugars
-
-
?
dinucleoside monophosphates + H2O
mononucleoside 5'-phosphate
-
2'-5' linkage
-
-
?
dinucleoside monophosphates + H2O
mononucleoside 5'-phosphate
-
3'-5' linkage
-
?
dinucleoside monophosphates + H2O
mononucleoside 5'-phosphate
-
-
-
-
?
dinucleoside monophosphates + H2O
mononucleoside 5'-phosphate
-
-
-
-
?
dinucleoside polyphosphate + H2O
?
-
-
-
-
?
dinucleoside polyphosphate + H2O
?
-
-
-
-
?
dinucleotides + H2O
?
-
3'-hydroxyl-terminated 3'-5'and 2'-5' linkage without specificity toward bases or sugars
-
-
?
dinucleotides + H2O
?
-
-
-
-
?
dinucleotides + H2O
?
-
-
-
-
?
DNA + H2O
DNA(n-1) + 2'-deoxynucleoside 5'-phosphate
-
-
-
-
?
DNA + H2O
DNA(n-1) + 2'-deoxynucleoside 5'-phosphate
-
denatured DNA. Native DNA is resistant
-
-
?
DNA + H2O
DNA(n-1) + 2'-deoxynucleoside 5'-phosphate
-
-
-
-
?
DNA + H2O
DNA(n-1) + 2'-deoxynucleoside 5'-phosphate
-
denatured DNA. Native DNA is resistant
-
-
?
DNA + H2O
DNA(n-1) + 2'-deoxynucleoside 5'-phosphate
-
-
-
-
?
DNA + H2O
DNA(n-1) + 2'-deoxynucleoside 5'-phosphate
-
enzyme hydrolyzes single-stranded DNA, no activity with double-stranded DNA
-
-
?
DNA + H2O
DNA(n-1) + 2'-deoxynucleoside 5'-phosphate
-
-
-
-
?
DNA + H2O
DNA(n-1) + 2'-deoxynucleoside 5'-phosphate
-
PC-1
-
-
?
DNA + H2O
DNA(n-1) + 2'-deoxynucleoside 5'-phosphate
-
enzyme hydolyzes single-stranded DNA more preferentially than double-stranded DNA, the enzyme also hydrolyzes nicked superhelical covalently closed circular phiX174RFI DNA to yield first open circular DNA and then linear DNA
-
-
?
DNA + H2O
DNA(n-1) + 2'-deoxynucleoside 5'-phosphate
-
enzyme hydrolyzes single-stranded DNA, no activity with double-stranded DNA
-
-
?
DNA + H2O
DNA(n-1) + 2'-deoxynucleoside 5'-phosphate
-
-
-
-
?
DNA + H2O
DNA(n-1) + 2'-deoxynucleoside 5'-phosphate
-
denatured DNA. Native DNA is resistant
-
-
?
DNA + H2O
DNA(n-1) + 2'-deoxynucleoside 5'-phosphate
-
native and denatured DNA
-
-
?
DNA + H2O
DNA(n-1) + 2'-deoxynucleoside 5'-phosphate
-
-
-
-
?
DNA + H2O
DNA(n-1) + 2'-deoxynucleoside 5'-phosphate
-
-
-
?
DNA + H2O
DNA(n-1) + 2'-deoxynucleoside 5'-phosphate
-
PC-1
-
-
?
DNA + H2O
DNA(n-1) + 2'-deoxynucleoside 5'-phosphate
-
enzyme hydrolyzes single-stranded DNA, no activity with double-stranded DNA
-
-
?
DNA + H2O
DNA(n-1) + 2'-deoxynucleoside 5'-phosphate
-
-
-
-
?
DNA + H2O
DNA(n-1) + 2'-deoxynucleoside 5'-phosphate
-
immobilized enzyme: not a substrate
-
-
?
DNA + H2O
DNA(n-1) + 2'-deoxynucleoside 5'-phosphate
-
-
-
-
?
DNA + H2O
DNA(n-1) + 2'-deoxynucleoside 5'-phosphate
-
heat-denatured: very slowly, native DNA is not hydrolyzed
-
-
?
NAD+ + H2O
5'-AMP + NMN
-
-
-
?
NAD+ + H2O
5'-AMP + NMN
-
slowly
-
-
?
NAD+ + H2O
5'-AMP + NMN
-
calf
-
?
NAD+ + H2O
5'-AMP + NMN
-
pyrophosphatase activity
-
-
?
NAD+ + H2O
5'-AMP + NMN
-
-
-
?
NAD+ + H2O
5'-AMP + NMN
-
-
-
?
NAD+ + H2O
5'-AMP + NMN
-
-
-
-
?
NAD+ + H2O
5'-AMP + NMN
-
-
-
-
?
NAD+ + H2O
5'-AMP + NMN
-
-
-
?
NAD+ + H2O
5'-AMP + NMN
-
-
-
-
?
NAD+ + H2O
5'-AMP + NMN
-
pyrophosphatase activity
-
?
NADP+ + H2O
NAD+ + phosphate
-
-
-
-
?
NADP+ + H2O
NAD+ + phosphate
-
-
-
?
oligonucleotides + H2O
oligonucleotides(n-1) + 5'-mononucleotides
-
-
-
-
?
oligonucleotides + H2O
oligonucleotides(n-1) + 5'-mononucleotides
-
-
-
-
?
oligonucleotides + H2O
oligonucleotides(n-1) + 5'-mononucleotides
-
specific for 3'-5'-direction from the 3'-hydroxyl terminal in a stepwise manner
-
?
oligonucleotides + H2O
oligonucleotides(n-1) + 5'-mononucleotides
-
-
-
?
oligonucleotides + H2O
oligonucleotides(n-1) + 5'-mononucleotides
-
specific for 3'-5'-direction from the 3'-hydroxyl terminal in a stepwise manner
-
-
?
oligonucleotides + H2O
oligonucleotides(n-1) + 5'-mononucleotides
-
specific for 3'-5'-direction from the 3'-hydroxyl terminal in a stepwise manner
-
?
oligonucleotides + H2O
oligonucleotides(n-1) + 5'-mononucleotides
-
PC-1
-
-
?
oligonucleotides + H2O
oligonucleotides(n-1) + 5'-mononucleotides
-
specific for 3'-5'-direction from the 3'-hydroxyl terminal in a stepwise manner
-
?
oligonucleotides + H2O
oligonucleotides(n-1) + 5'-mononucleotides
-
-
-
?
oligonucleotides + H2O
oligonucleotides(n-1) + 5'-mononucleotides
-
-
-
?
oligonucleotides + H2O
oligonucleotides(n-1) + 5'-mononucleotides
-
PC-1
-
-
?
oligonucleotides + H2O
oligonucleotides(n-1) + 5'-mononucleotides
-
-
-
-
?
oligonucleotides + H2O
oligonucleotides(n-1) + 5'-mononucleotides
-
specific for 3'-5'-direction from the 3'-hydroxyl terminal in a stepwise manner
-
?
oligonucleotides + H2O
oligonucleotides(n-1) + 5'-mononucleotides
-
specific for 3'-5'-direction from the 3'-hydroxyl terminal in a stepwise manner
-
?
oligonucleotides + H2O
oligonucleotides(n-1) + 5'-mononucleotides
-
specific for 3'-5'-direction from the 3'-hydroxyl terminal in a stepwise manner
-
-
?
p-nitrophenyl 5'-thymidine monophosphate + H2O
p-nitrophenol + 5'-thymidine monophosphate
-
-
-
?
p-nitrophenyl 5'-thymidine monophosphate + H2O
p-nitrophenol + 5'-thymidine monophosphate
-
-
-
-
?
p-nitrophenyl phenylphosphonate + H2O
p-nitrophenol + benzenephosphonic acid
-
-
-
-
?
p-nitrophenyl phenylphosphonate + H2O
p-nitrophenol + benzenephosphonic acid
-
-
-
-
?
p-nitrophenyl phenylphosphonate + H2O
p-nitrophenol + benzenephosphonic acid
-
-
-
-
?
p-nitrophenyl phenylphosphonate + H2O
p-nitrophenol + benzenephosphonic acid
-
-
-
-
?
p-nitrophenylphosphorylcholine + H2O
p-nitrophenol + phosphorylcholine
-
-
-
?
p-nitrophenylphosphorylcholine + H2O
p-nitrophenol + phosphorylcholine
-
-
-
?
p-nitrophenylthymidine 5'-phosphate + H2O
5'-TMP + p-nitrophenol
-
-
-
-
?
p-nitrophenylthymidine 5'-phosphate + H2O
5'-TMP + p-nitrophenol
-
-
-
-
?
p-nitrophenylthymidine 5'-phosphate + H2O
5'-TMP + p-nitrophenol
-
-
-
-
?
p-nitrophenylthymidine 5'-phosphate + H2O
5'-TMP + p-nitrophenol
-
-
-
-
?
p-nitrophenylthymidine 5'-phosphate + H2O
5'-TMP + p-nitrophenol
-
-
-
-
?
p-nitrophenylthymidine 5'-phosphate + H2O
5'-TMP + p-nitrophenol
-
-
-
-
?
p-nitrophenylthymidine 5'-phosphate + H2O
5'-TMP + p-nitrophenol
-
-
-
-
?
p-nitrophenylthymidine 5'-phosphate + H2O
5'-TMP + p-nitrophenol
-
-
-
-
?
p-nitrophenylthymidine 5'-phosphate + H2O
5'-TMP + p-nitrophenol
-
-
-
-
?
p-nitrophenylthymidine 5'-phosphate + H2O
5'-TMP + p-nitrophenol
-
-
-
-
?
p-nitrophenylthymidine 5'-phosphate + H2O
5'-TMP + p-nitrophenol
-
-
-
-
?
p-nitrophenylthymidine 5'-phosphate + H2O
5'-TMP + p-nitrophenol
-
-
-
-
?
p-nitrophenylthymidine 5'-phosphate + H2O
5'-TMP + p-nitrophenol
-
-
-
-
?
p-nitrophenylthymidine 5'-phosphate + H2O
5'-TMP + p-nitrophenol
-
-
-
-
?
p-nitrophenylthymidine 5'-phosphate + H2O
5'-TMP + p-nitrophenol
-
PC-1
-
-
?
p-nitrophenylthymidine 5'-phosphate + H2O
5'-TMP + p-nitrophenol
-
-
-
-
?
poly A + H2O
5'-AMP
-
-
-
-
?
poly A + H2O
5'-AMP
-
-
-
?
poly A + H2O
5'-AMP
-
-
-
?
poly C + H2O
5'-CMP
-
-
-
-
?
poly C + H2O
5'-CMP
-
-
-
?
poly U + H2O
5'-UMP
-
-
-
-
?
poly U + H2O
5'-UMP
-
-
-
?
poly U + H2O
5'-UMP
-
-
-
?
poly(I) + H2O
5'-IMP
-
slowly
-
-
?
poly(I) + H2O
5'-IMP
-
-
-
?
polynucleotides + H2O
polynucleotides(n-1) + 5'-mononucleotides
-
specific for 3'-5'-direction from the 3'-hydroxyl terminal in a stepwise manner
-
?
polynucleotides + H2O
polynucleotides(n-1) + 5'-mononucleotides
-
specific for 3'-5'-direction from the 3'-hydroxyl terminal in a stepwise manner
-
-
?
polynucleotides + H2O
polynucleotides(n-1) + 5'-mononucleotides
-
-
-
-
?
polynucleotides + H2O
polynucleotides(n-1) + 5'-mononucleotides
-
specific for 3'-5'-direction from the 3'-hydroxyl terminal in a stepwise manner
-
-
?
polynucleotides + H2O
polynucleotides(n-1) + 5'-mononucleotides
-
specific for 3'-5'-direction from the 3'-hydroxyl terminal in a stepwise manner
-
-
?
polynucleotides + H2O
polynucleotides(n-1) + 5'-mononucleotides
-
specific for 3'-5'-direction from the 3'-hydroxyl terminal in a stepwise manner
-
?
polynucleotides + H2O
polynucleotides(n-1) + 5'-mononucleotides
-
PC-1
-
-
?
polynucleotides + H2O
polynucleotides(n-1) + 5'-mononucleotides
-
specific for 3'-5'-direction from the 3'-hydroxyl terminal in a stepwise manner
-
?
polynucleotides + H2O
polynucleotides(n-1) + 5'-mononucleotides
-
specific for 3'-5'-direction from the 3'-hydroxyl terminal in a stepwise manner
-
-
?
polynucleotides + H2O
polynucleotides(n-1) + 5'-mononucleotides
-
-
-
?
polynucleotides + H2O
polynucleotides(n-1) + 5'-mononucleotides
-
-
-
?
polynucleotides + H2O
polynucleotides(n-1) + 5'-mononucleotides
-
PC-1
-
-
?
polynucleotides + H2O
polynucleotides(n-1) + 5'-mononucleotides
-
specific for 3'-5'-direction from the 3'-hydroxyl terminal in a stepwise manner
-
-
?
polynucleotides + H2O
polynucleotides(n-1) + 5'-mononucleotides
-
very slowly
-
-
?
polynucleotides + H2O
polynucleotides(n-1) + 5'-mononucleotides
-
specific for 3'-5'-direction from the 3'-hydroxyl terminal in a stepwise manner
-
-
?
RNA + H2O
RNA(n-1) + nucleoside 5'-phosphate
-
-
-
-
?
RNA + H2O
RNA(n-1) + nucleoside 5'-phosphate
-
highly polymerized RNA: hydrolyzed at medium speed, single-stranded RNA: slowly, tRNA: not a substrate
-
-
?
RNA + H2O
RNA(n-1) + nucleoside 5'-phosphate
-
RNase J1 activity is sensitive to the phosphorylation state of the 5'-end, with severalfold greater activity observed with monophosphorylated or hydroxylated 5'-ends than with triphosphorylated 5'-ends
-
-
?
RNA + H2O
RNA(n-1) + nucleoside 5'-phosphate
-
RNase J1 activity is sensitive to the phosphorylation state of the 5'-end, with severalfold greater activity observed with monophosphorylated or hydroxylated 5'-ends than with triphosphorylated 5'-ends
-
-
?
RNA + H2O
RNA(n-1) + nucleoside 5'-phosphate
-
-
-
-
?
RNA + H2O
RNA(n-1) + nucleoside 5'-phosphate
-
calf, only single-stranded portion of tRNA from 3'-OH end
-
-
?
RNA + H2O
RNA(n-1) + nucleoside 5'-phosphate
-
-
-
-
?
RNA + H2O
RNA(n-1) + nucleoside 5'-phosphate
-
-
-
-
?
RNA + H2O
RNA(n-1) + nucleoside 5'-phosphate
-
PC-1
-
-
?
RNA + H2O
RNA(n-1) + nucleoside 5'-phosphate
-
-
-
-
?
RNA + H2O
RNA(n-1) + nucleoside 5'-phosphate
-
PC-1
-
-
?
RNA + H2O
RNA(n-1) + nucleoside 5'-phosphate
-
-
-
-
?
RNA + H2O
RNA(n-1) + nucleoside 5'-phosphate
-
-
-
-
?
RNA + H2O
RNA(n-1) + nucleoside 5'-phosphate
-
very slowly
-
-
?
UDP-glucose + H2O
glucose-1-phosphate + 5'-UMP
-
-
-
?
UDP-glucose + H2O
glucose-1-phosphate + 5'-UMP
-
PC-1
PC-1
?
UDP-glucose + H2O
glucose-1-phosphate + 5'-UMP
-
-
-
-
?
additional information
?
-
AtTDP has Tyr-phosphodiesterase activity for the topoisomerase-DNA complex
-
-
?
additional information
?
-
-
no activity with dinucleotides bearing 3'-phosphate , 2': 3'-cyclic AMP and 3': 5'-cyclic AMP
-
-
?
additional information
?
-
-
no activity with 2',3'-cyclic nucleotides
-
-
?
additional information
?
-
-
enzyme does not have a strict base specificity, it does not attack oligonucleotides with a 3'-phosphate terminal
-
-
?
additional information
?
-
-
broad substrate specificity
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
no activity with the cyclic trimer of deoxythymidine 5'-phosphate and adenosine 3',5'-monophosphate
-
-
?
additional information
?
-
-
new definition for PDE I activity which takes into account its ability to hydrolyze several types of substrates
-
-
?
additional information
?
-
-
no activity with p-nitrophenylthymidine 3'-phosphate
-
-
?
additional information
?
-
-
no activity with p-nitrophenylthymidine 3'-phosphate
-
-
?
additional information
?
-
-
study on substrate specificity and structural requirements using synthetic oligonucleotide derivatives suitable for labeling of nucleic acids
-
?
additional information
?
-
-
the enzyme may be important in nucleotide metabolism on the cell surface
-
-
?
additional information
?
-
E2REL5
substrates are protein-DNA adducts, such as camptothecin stabilized Topo1-DNA adducts, and modified nucleotides, including oxidized nucleotides and chain terminating nucleoside analogues
-
-
?
additional information
?
-
-
study on substrate specificity and structural requirements using synthetic oligonucleotide derivatives suitable for labeling of nucleic acids
-
?
additional information
?
-
-
substrate specificity and structural requirements
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
substrates are protein-DNA adducts, such as camptothecin stabilized Topo1-DNA adducts, and modified nucleotides, including oxidized nucleotides and chain terminating nucleoside analogues
-
-
?
additional information
?
-
-
no activity with cyclic nucleotides such as 2',3'-cyclic AMP, 3',5'-cyclic AMP, or 3',5'-cyclic GMP
-
-
?
additional information
?
-
substrates are protein-DNA adducts, such as camptothecin stabilized Topo1-DNA adducts, and modified nucleotides, including oxidized nucleotides and chain terminating nucleoside analogues
-
-
?
additional information
?
-
-
no activity with p-nitrophenylthymidine 3'-phosphate
-
-
?
additional information
?
-
-
no activity with p-nitrophenylthymidine 3'-phosphate
-
-
?
additional information
?
-
-
broad substrate specificity
-
-
?
additional information
?
-
-
PC-1, PC-1 may take part in purine uptake for metabolic needs of cells
-
-
?
additional information
?
-
-
enzyme might function as a modulating factor of platelet aggregation
-
-
?
additional information
?
-
-
enzyme may be involved in nucleotides metabolism in human plasma
-
-
?
additional information
?
-
-
PC-1 plays a major role in bone and cartilage metabolism by producing diphosphate
-
-
?
additional information
?
-
-
tyrosyl-DNA phosphodiesterase 1 catalyses the hydrolysis of phosphodiester linkages between a DNA 3' phosphate and a tyrosine residue as well as a variety of other DNA 3 substituents, the enzyme shows affinity for the substrate increased as the DNA length
-
-
?
additional information
?
-
-
Tdp1 activity on DNA substrate with 3'-dRP moiety in the single strand break. The 15-mer with 3'-dRP is generated by incubating 10 nM AP-DNA with EndoIII, site cleavage activity of tyrosyl-DNA phosphodiesterase 1, overview
-
-
?
additional information
?
-
-
the active site H263 is covalently bound through a phosphoamide bond to the 3' end of DNA moiety of the substrate
-
-
?
additional information
?
-
SMPDL3A is a functional metallophosphoesterase, and despite having no detectable activity towards sphingomyelin, possesses a nucleotide phosphodiesterase activity, particularly strongly against nucleotide triphosphates
-
-
?
additional information
?
-
-
SMPDL3A is a functional metallophosphoesterase, and despite having no detectable activity towards sphingomyelin, possesses a nucleotide phosphodiesterase activity, particularly strongly against nucleotide triphosphates
-
-
?
additional information
?
-
substrates are protein-DNA adducts, such as camptothecin stabilized Topo1-DNA adducts, and modified nucleotides, including oxidized nucleotides and chain terminating nucleoside analogues, substrates vary in size and complexity
-
-
?
additional information
?
-
-
the enzyme catalyzes the hydrolysis of 3' phosphotyrosyl linkers and other 3'-end blocking lesions. When Top1 nicks double-stranded DNA, a covalent cleavage complex is formed that can be repaired by the enzyme, the mechanism involves the following steps: first, as Lys265 and Lys495 residues in the catalytic site coordinate the oxygen atoms of the phosphate group, His263 attacks the phosphorus atom linked to the oxygen of the Top1 catalytic residue, Tyr723, at the 3' end of DNA. Second, the TDP1-DNA covalent intermediate formed is hydrolyzed by a His493-activated water molecule, leading to the generation of a DNA product with a 3' phosphate
-
-
?
additional information
?
-
-
the enzyme cleaves the apurinic/apyrimidinic site in DNA by hydrolysis of the phosphodiester bond between the substituent and 5' adjacent phosphate. The product of enzyme cleavage in the case of the apurinic/apyrimidinic site is unstable and is hydrolyzed with the formation of 3'- and 5'-margin phosphates. The following repair demands the ordered action of polynucleotide kinase phosphorylase, with XRCC1, DNA polymerase beta, and DNA ligase, mechanism, overview
-
-
?
additional information
?
-
-
tyrosyl-DNA phosphodiesterase 1 catalyzes the hydrolysis of the phosphodiester linkage between the DNA 3'-phosphate and a tyrosine residue as well as a variety of other DNA 30 damaged termini. The enzyme can liberate the 3'-DNA phosphate termini from apurinic/apyrimidinic sites. The enzyme is more active in the cleavage of the apurinic/apyrimidinic sites inside bubble-DNA structure in comparison to ssDNA containing apurinic/apyrimidinic site, it hydrolyzes apurinic/apyrimidinic sites opposite to bulky fluorescein adduct faster than apurinic/apyrimidinic sites located in dsDNA, specificity of the apurinic/apyrimidinic site cleavage activity
-
-
?
additional information
?
-
-
tyrosyl-DNA phosphodiesterase I specifically catalyzes the hydrolysis of the phosphodiester bond between the catalytic Tyr723 of Top1 and DNA-3'-phosphate, then polynucleotide kinase phosphatase hydrolyzes the resulting 3'-phosphate end and catalyzes the phosphorylation of the 5'-hydroxyl end of the broken DNA strand. This results in a broken DNA strand with termini consisting of a 5'-phosphate and 3'-hydroxyl for DNA repair. DNA polymerase beta replaces the missing DNA segment, and finally DNA ligase III reseals the broken DNA
-
-
?
additional information
?
-
-
efficiency of apurinic/apyrimidinic site hydrolysis catalyzed by the enzyme decreases in the order: dsAP-DNA/bubble > ssAP-DNA > dsAP-DNA/Flu >> dsAP-DNA, the enzyme shows preference for 3'-substituent located on the termini of DNA compared to nicks
-
-
?
additional information
?
-
-
isozymes NPP1 and NPP3 can hydrolyze ATP, as well as inhibitor molecule 4, they also show very low activity with inhibitors 1 and 2, 1-4% compared to the activit with ATP
-
-
?
additional information
?
-
-
recombinant human enzyme processes 5'-phosphotyrosyl DNA ends when they mimic the 5'-overhangs of topoisomerase II-DNA cleavage complexes and 3'-deoxyribose phosphates generated from hydrolysis of abasic sites
-
-
?
additional information
?
-
SMPDL3A is not an acid sphingomyelinase, but unexpectedly is active against nucleotide diphosphate and triphosphate substrates at acidic and neutral pH
-
-
?
additional information
?
-
-
SMPDL3A is not an acid sphingomyelinase, but unexpectedly is active against nucleotide diphosphate and triphosphate substrates at acidic and neutral pH
-
-
?
additional information
?
-
-
substrate is 5'-[32P]-labeled single-stranded DNA oligonucleotide containing a 3'-phosphotyrosine (N14Y)
-
-
?
additional information
?
-
-
substrate is a 5'-[32P]-labeled single-stranded DNA oligonucleotide containing a 3' phosphotyrosine (N14Y)
-
-
?
additional information
?
-
the enzyme is able to act as a limited 3'-exonuclease by removing a single RNA or DNA nucleotide from the 3'-end of the DNA, but only if it bears a 3'-hydroxyl-group rather than a 3'-phosphoryl-group. The latter restriction prevents the enzyme from acting as a classic endonuclease to degrade the products of its own catalysis
-
-
?
additional information
?
-
-
the enzyme is also able to effectively cleave non-nucleotide insertions in DNA, decanediol and diethyleneglycol moieties by the same mechanism as in the case of tetrahydrofuran cleavage, it catalyzes the hydrolysis of decanediol- and bis-ethylene glycol-containing DNA even more effectively than tetrahydrofuran-containing DNA particularly in the case of decanediol-containing DNA. Repair of 5'-tetrahydrofuran and other apurinic/apyrimidinic site analogues can be processed by the long-patch base excision repair pathway, overview.The efficiency of enzyme-catalyzed hydrolysis of apurinic/apyrimidinic-site analogues correlates with the DNA helix distortion induced by the substituent
-
-
?
additional information
?
-
the enzyme cleaves the 3'-diester bond between tyrosine and DNA as well as removes other lesions, producing a 3'-phosphate that can be removed by polynucleotide kinase/phosphatase
-
-
?
additional information
?
-
the enzyme hydrolyzes the phosphodiester bond between a catalytic tyrosine Tyr723 (human) of topoisomerase 1 and DNA 3'-phosphate
-
-
?
additional information
?
-
-
the physiological function of PDE in plant cell is presumably the degradation of nucleic acids
-
-
?
additional information
?
-
-
no activity with dinucleotides bearing 3'-phosphate , 2': 3'-cyclic AMP and 3': 5'-cyclic AMP
-
-
?
additional information
?
-
-
no activity with p-nitrophenylthymidine 3'-phosphate
-
-
?
additional information
?
-
-
no activity with dinucleotides bearing 3'-phosphate , 2': 3'-cyclic AMP and 3': 5'-cyclic AMP
-
-
?
additional information
?
-
-
no activity with p-nitrophenylthymidine 3'-phosphate
-
-
?
additional information
?
-
product of the reaction is a 3'-phosphate and not a 3'-hydroxyl
-
-
?
additional information
?
-
-
product of the reaction is a 3'-phosphate and not a 3'-hydroxyl
-
-
?
additional information
?
-
-
no activity with cAMP
-
-
?
additional information
?
-
-
broad substrate specificity
-
-
?
additional information
?
-
-
overview on substrate specificity
-
?
additional information
?
-
-
implication of enzyme in intra- and extracellular processes, overview
-
?
additional information
?
-
-
PC-1, PC-1 may take part in purine uptake for metabolic needs of cells
-
-
?
additional information
?
-
-
PC-1, PC-1 may take part in purine uptake for metabolic needs of cells
-
-
?
additional information
?
-
-
PC-1, nucleotide pyrophosphatase/alkaline phosphodiesterase I, may have a role in the regulation of N-linked glycosylation, it may regulate the availability of nucleotide sugar precusors at the site of oligosaccharide synthesis
-
-
?
additional information
?
-
substrates are protein-DNA adducts, such as camptothecin stabilized Topo1-DNA adducts, and modified nucleotides, including oxidized nucleotides and chain terminating nucleoside analogues
-
-
?
additional information
?
-
-
PC-1, nucleotide pyrophosphatase/alkaline phosphodiesterase I, may have a role in the regulation of N-linked glycosylation, it may regulate the availability of nucleotide sugar precusors at the site of oligosaccharide synthesis
-
-
?
additional information
?
-
NPP1 exhibits hydrolytic activity toward ADP-glucose and plastid-targeting ability
-
-
?
additional information
?
-
NPP1 exhibits hydrolytic activity toward ADP-glucose and plastid-targeting ability
-
-
?
additional information
?
-
unlike isozyme NPP1, isozyme NPP3 exhibits no hydrolytic activity toward ADP-glucose and no plastid-targeting ability
-
-
?
additional information
?
-
unlike isozyme NPP1, isozyme NPP3 exhibits no hydrolytic activity toward ADP-glucose and no plastid-targeting ability
-
-
?
additional information
?
-
-
broad substrate specificity
-
-
?
additional information
?
-
-
no activity with cAMP
-
-
?
additional information
?
-
-
no activity with dinucleotides bearing 3'-phosphate
-
-
?
additional information
?
-
-
enzyme does not have a strict base specificity, it does not attack oligonucleotides with a 3'-phosphate terminal
-
-
?
additional information
?
-
-
no activity with UTP and UDP
-
-
?
additional information
?
-
-
no activity with p-nitrophenylthymidine 3'-phosphate
-
-
?
additional information
?
-
-
broad substrate specificity
-
-
?
additional information
?
-
-
broad substrate specificity
-
-
?
additional information
?
-
-
phosphodiesterase activity results in the cleavage of nucleotides from nucleic acids and thus may be involved in catabolism of extracellular DNA. Essential function may be to hydrolyze polyribo- and polydeoxyribonucleotides. The enzyme may be important in cell differentiation during carcinogenesis
-
-
?
additional information
?
-
-
PC-1, plasma-membrane-associated enzyme with nucleotide pyrophosphatase/phosphodiesterase I activity is probably involved in the clearance of extracellular nucleotides such as ATP and diadenosine polyphosphates
-
-
?
additional information
?
-
-
isoform NPP1 is involved in cleavage of extracellular diadenosine polyphosphates in brain
-
-
?
additional information
?
-
substrates are protein-DNA adducts, such as camptothecin stabilized Topo1-DNA adducts, and modified nucleotides, including oxidized nucleotides and chain terminating nucleoside analogues
-
-
?
additional information
?
-
-
PMH hydrolyses phosphonate monoesters and phosphate diesters with similar efficiency
-
-
?
additional information
?
-
substrates are protein-DNA adducts, such as camptothecin stabilized Topo1-DNA adducts, and modified nucleotides, including oxidized nucleotides and chain terminating nucleoside analogues, substrates vary in size and complexity
-
-
?
additional information
?
-
the enzyme hydrolyzes the covalent bond between the tyrosyl residue of topoisomerase 1 and the 3'-phosphate group in DNA. The enzyme is able to initiate the cleavage of internal apurinic/apyrimidinic sites or 3-hydroxy-2-hydroxymethyl tetrahydrofuran in DNA and its subsequent repair
-
-
?
additional information
?
-
-
the enzyme hydrolyzes the covalent bond between the tyrosyl residue of topoisomerase 1 and the 3'-phosphate group in DNA. The enzyme is able to initiate the cleavage of internal apurinic/apyrimidinic sites or 3-hydroxy-2-hydroxymethyl tetrahydrofuran in DNA and its subsequent repair
-
-
?
additional information
?
-
substrates are protein-DNA adducts, such as camptothecin stabilized Topo1-DNA adducts, and modified nucleotides, including oxidized nucleotides and chain terminating nucleoside analogues, substrates vary in size and complexity
-
-
?
additional information
?
-
-
no activity with dinucleotides bearing 3'-phosphate
-
-
?
additional information
?
-
-
enzyme does not have a strict base specificity, it does not attack oligonucleotides with a 3'-phosphate terminal
-
-
?
additional information
?
-
-
no activity with p-nitrophenylthymidine 3'-phosphate
-
-
?
additional information
?
-
-
no activity with p-nitrophenylthymidine 3'-phosphate
-
-
?
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(2R,4R,4aR,7R,8aS)-4,7-dimethyl-2-(5-aminothiophen-2-yl)octahydro-2H-chromen-4-ol
-
(2R,4S,4aR,7R,8aS)-4,7-dimethyl-2-(5-aminothiophen-2-yl)octahydro-2H-chromen-4-ol
-
(5Z)-5-(2,3,4-trihydroxybenzylidene)-1,3-thiazolidine-2,4-dithione
-
-
(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]-isoquinolin-3-yl)carbamic acid
-
-
(RP)-adenosine 5'-(alpha-thio-beta,gamma-dichloromethylene)triphosphate
-
-
(RP)-adenosine 5'-(alpha-thio-beta,gamma-methylene)triphosphate
-
-
(S)-3-(4-hydroxy-3-methoxyphenyl)propane-1,2-diol-2-beta-D-(6'-O-galloyl) glucopyranoside
-
(SP)-adenosine 5'-(alpha-thio-beta,gamma-dichloromethylene)triphosphate
-
-
(SP)-adenosine 5'-(alpha-thio-beta,gamma-methylene)triphosphate
-
-
1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one
1,2-dimethyl-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
10,12-dibromo-1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
10,12-dibromo-1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
10,12-dibromo-1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
10,12-dibromo-1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
10,12-dibromo-1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
10,12-dibromo-3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
10,12-dibromo-3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
10-bromo-1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
10-bromo-1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
10-bromo-1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
10-bromo-1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
10-bromo-1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
10-bromo-3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
10-bromo-3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
11,13-dibromo-1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one
11-bromo-1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one
2,2,2-trifluoro-N-(5-((2R,4R,4aR,7R,8aR)-4-hydroxy-4,7-dimethyloctahydro-2H-chromen-2-yl)thiophen-2-yl)acetamide
-
2,2,2-trifluoro-N-(5-((2R,4S,4aR,7R,8aR)-4-hydroxy-4,7-dimethyloctahydro-2H-chromen-2-yl)thiophen-2-yl)acetamide
-
2,2,2-trifluoro-N-(8-(trifluoromethyl)benzo[f][1,2,3,4,5]pentathiepin-6-yl)acetamide
-
2-((6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino)acetic acid
-
-
2-(2,6-dimethylhept-5-en-1-yl)-5,7-dimethyl-1,3-diazatricyclo[3.3.1.1(3,7)]decan-6-one
-
2-(3-(dimethylamino)propoxy)-3-methoxy-6-(3-morpholinopropyl)-5H-[1,3]dioxolo[4',5':5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
-
-
2-(3-(ethylamino)propoxy)-3-methoxy-6-(3-morpholinopropyl)-5H-[1,3]dioxolo[4',5':5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
-
-
2-(3-aminopropoxy)-3-methoxy-6-(3-morpholinopropyl)-5H-[1,3]dioxolo[4',5':5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
-
-
2-(dibutylamino)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide
-
2-(piperidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide
-
2-(pyrrolidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide
-
2-crotonyloxymethyl-(4R,5R,6R)-trihydroxy-cyclohex-2-enone
-
tumor cell line
2-morpholino-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide
-
3,20-dioxopregn-4-en-21-yl 4-bromobenzene-1-sulfonate
-
3,20-dioxopregn-4-en-21-yl 4-bromobenzenesulfonate
-
-
3,4-dimethoxyphenol-1-beta-D-(6'-O-galloyl)glucopyranoside
-
3-(((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one
-
3-(((1S,5R)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one
-
3-((3,4,5-trimethoxybenzyl)oxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one
-
3-((3-methoxybenzyl)oxy)-7,8,9,10-tetrahydro-6Hbenzo[c]chromen-6-one
-
3-(2-((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)ethoxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one
-
3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
3-(4-hydroxy-3-methoxyphenyl)propane-1,2-diol 2-beta-D-(6'-O-galloyl)glucopyranoside
-
3-(4-methoxy-phenyl)-1-(3-nitro-phenyl)-8Hpyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
3-(benzyloxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one
-
3-(piperidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)propanamide
-
3-(pyrrolidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)propanamide
-
3-amino-6-(3-aminopropyl)-5,6-dihydro-9-methoxy-5,11-dioxo-11H-indeno[1,2-c]isoquinoline dihydrochloride
-
-
3-amino-6-(3-aminopropyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
3-cyano-6,11-dihydro-5,11-dioxo-6-[3-(dimethylaminopropyl)-5H-indeno[1,2-c]isoquinoline]
-
-
3-iodo-9-methoxy-6-(3-(dimethylamino)propyl)-5H-indeno-[1,2-c]isoquinoline-5,11(6H)-dione
-
-
3-isobutyl-1-methyl xanthine
-
-
3-isobutyl-1-methylxanthine
-
i.e. IBMX
3-methoxy-6-(3-morpholinopropyl)-2-(3-(piperidin-1-yl)-propoxy)-5H-[1,3]dioxolo[4',5':5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
-
-
3-methoxy-6-(3-morpholinopropyl)-2-(3-(pyrrolidin-1-yl)-propoxy)-5H-[1,3]dioxolo[4',5':5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione
-
-
3-morpholino-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)propanamide
-
4,4'-(furan-2,5-diyl)di(benzene-1-carboximidamide)
-
4-methyl-7-((3,4,5-trimethoxybenzyl)oxy)-2H-chromen-2-one
-
4-[(6-(3-((tert-butoxycarbonyl)amino)propyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl)amino]-4-oxobutanoic acid
-
-
5'-deoxyribonucleotides
-
5-[3-benzyloxyphenyl]-1,3,4-oxadiazole-2(3H)-thione
5-[3-hydroxyphenyl]-1,3,4-oxadiazole-2(3H)-thione
-
-
5-[4-(t-butyldimethylsilyloxy)-phenyl]-1,3,4-oxadiazole-2(3H)-thione
5-[4-(t-butyldimethylsilyloxy)-phenyl]-1,3,4-thiadiazole-2(3H)-thione
-
-
5-[4-benzyloxyphenyl]-1,3,4-oxadiazole-2(3H)-thione
5-[4-benzyloxyphenyl]-3-octyl-1,3,4-oxadiazole-2(3H)-thione
-
-
5-[4-hydroxyphenyl]-1,3,4-oxadiazole-2(3H)-thione
-
-
5-[4-hydroxyphenyl]-1,3,4-thiadiazole-2(3H)-thione
5-[4-pyridyl]-1,3,4-oxadiazole-2(3H)-thione
-
-
5-[4-pyridyl]-1,3,4-thiadiazole-2(3H)-thione
6,6'-[(1R,2R,3S,4S)-2,4-bis(4-hydroxyphenyl)cyclobutane-1,3-diyl]di(2H-pyran-2-one)
-
6,6'-[propane-1,3-diylbis(iminopropane-3,1-diyl)]bis(5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione)
-
-
6-(10-aminodecyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(11-aminoundecyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(12-aminododecyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(2-aminoethyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(3-(1H-imidazol-1-yl)propyl)-8-methoxy-3-nitro-5Hindeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(3-aminopropyl)-3-(methylamino)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(3-aminopropyl)-3-nitro-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(3-aminopropyl)-5,6-dihydro-8-methoxy-3-nitro-5,11-dioxo-11H-indeno[1,2-c]isoquinoline
-
-
6-(3-aminopropyl)-5,6-dihydro-9-methoxy-3-iodo-5,11-dioxo-11H-indeno[1,2-c]isoquinoline
-
-
6-(3-aminopropyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(3-aminopropyl)-7-methoxy-3-nitro-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(3-aminopropyl)-8-hydroxy-3-nitro-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
6-(3-aminopropyl)-9-methoxy-3-nitro-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(4-aminobutyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(5-aminopentyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(6-aminohexyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(7-aminoheptyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(8-aminooctyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-(9-aminononyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
-
-
6-[(6-(3-((tert-butoxycarbonyl)amino)propyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl)amino]-6-oxohexanoic acid
-
-
7-(((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
-
7-(((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-4-methyl-2H-chromen-2-one
-
7-(((1S,5R)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
-
7-(((1S,5R)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-4-methyl-2H-chromen-2-one
-
7-((3,4,5-trimethoxybenzyl)oxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
-
7-((3-methoxybenzyl) oxy)-4-methyl-2H-chromen-2-one
-
7-((3-methoxybenzyl)oxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
-
7-(2-((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)ethoxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
-
7-(benzyloxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
-
7-(benzyloxy)-4-methyl-2H-chromen-2-one
-
7-[[(1S,5R)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl]methoxy]-2,3-dihydrobenzo[b]cyclopenta[d]pyran-4(1H)-one
-
8-methoxymethyl isobutylmethylxanthine
-
20 microM, 8-MM-IBMX, a selective PDE1 inhibitor, no effect on either JG cell cAMP content or renin release compared to untreated controls
8-thioadenosine 5'-triphosphate
-
-
9,11-dibromo-1,2-dimethyl-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
9,11-dibromo-1-(2-furyl)-3-(4-tolyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
9,11-dibromo-1-(4-chlorophenyl)-3-(4-tolyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
9,11-dibromo-1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
9,11-dibromo-1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
9,11-dibromo-1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
9,11-dibromo-1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
9-bromo-1,2-dimethyl-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
9-bromo-1-(4-chlorophenyl)-3-(4-tolyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
9-bromo-1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
9-bromo-1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
9-bromo-1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
adenosine 5'-(gamma-thio-beta,gamma-methylene)triphosphate
-
-
ADP-ribose
-
competitive to diuridine tetraphosphate
alpha,beta-methylene-adenosine triphosphate
-
inhibition in decreasing order: alpha,beta-methyl-adenosine triphosphate, ATP, UTP, GTP, CTP
alpha,beta-methylene-ADP
-
-
aminobenzopentathiepine
-
ascorbic acid
-
slight inhibition
beta,gamma-methylene-ATP
-
-
bis(1,3,4-oxadiazol-2-methyl)-5-thione
-
-
bis(1,3,4-oxadiazol-2-propyl)-5-thione
bis(1,3,4-thiadiazole-2-methyl)-5-thione
-
-
cAMP
-
3 mM, 86% residual activity
Citric acid
-
slight inhibition
CTP
-
inhibition in decreasing order: alpha,beta-methylene-adenosine triphosphate, ATP, UTP, GTP, CTP
cystine
-
slight inhibition
diadenosine polyphosphate
-
competitive
-
diisopropyl fluorophosphate
-
bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase
diphosphate
-
slight inhibition
dipyramidole
-
0.1 mM, inhibition, no inhibition at 0.003 mM
ethyl 2-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5Hindeno[1,2-c]isoquinolin-3-yl)amino]acetate
-
-
Fe2+
-
bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase
Fe3+
-
bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase, 50% inhibition
guanosine 5'-tetraphosphate
-
competitive
IC86340
-
a PDE1 inhibitor, significantly reduces collagen I in human saphenous vein explants undergoing spontaneous remodeling via ex vivo culture, and acts synergistically with bicarbonate, in the absence of bicarbonate of IC86340, itself has no effect on collagen I protein. PDE1C but not PDE1A is the major isoform responsible for mediating the effects of IC86340. Lysosome inhibitors,. i.e. 2',4'-dichlorobenzamil, a nonselective CNG channel blocker, and the more specific CNG channel blocker, L-cisdiltiazem, block IC86340-mediated collagen I reduction, overview
-
isobutylmethylxanthine
-
100 microM, a nonselective PDE1 inhibitor, increases cAMP and renin relase by 72% and 118%, respectively
KH2PO4
-
slight inhibition
methyl 2-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5Hindeno[1,2-c]isoquinolin-3-yl)amino]-2-oxoacetate
-
-
methyl 3-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5Hindeno[1,2-c]isoquinolin-3-yl)amino]-3-oxopropanoate
-
-
methyl 4-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5Hindeno[1,2-c]isoquinolin-3-yl)amino]-4-oxobutanoate
-
-
methyl 5-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5Hindeno[1,2-c]isoquinolin-3-yl)amino]-5-oxopentanoate
-
-
methyl 6-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5Hindeno[1,2-c]isoquinolin-3-yl)amino]-6-oxohexanoate
-
-
methyl-3,4-dephostatin
a dephostatin derivative, structure-activity relationship analogues of this active compound that have a chemical substitution at a single position show a dramatic decrease in inhibition activity
N-(2-[1-[2-(2-methyl-1H-imidazol-1-yl)pyrimidin-4-yl]piperidin-4-yl]ethyl)sulfuric diamide
-
-
N-(2-[1-[6-(2-methyl-1H-imidazol-1-yl)pyrimidin-4-yl]piperidin-4-yl]ethyl)sulfuric diamide
-
-
N-(3,7-dimethyloct-6-en-1-yl)tricyclo[3.3.1.1(3,7)]decan-2-amine
-
N-(5-((2R,4R,4aR,7R,8aR)-4-hydroxy-4,7-dimethyloctahydro-2H-chromen-2-yl)thiophen-2-yl)acetamide
-
N-(5-((2R,4R,4aR,7R,8aR)-4-hydroxy-4,7-dimethyloctahydro-2H-chromen-2-yl)thiophen-2-yl)benzamide
-
N-(5-((2R,4R,4aR,7R,8aS)-4-hydroxy-4,7-dimethyloctahydro-2H-chromen-2-yl)thiophen-2-yl)adamantane-1-carboxamide
-
N-(5-((2R,4S,4aR,7R,8aR)-4-hydroxy-4,7-dimethyloctahydro-2H-chromen-2-yl)thiophen-2-yl)acetamide
-
N-(5-((2R,4S,4aR,7R,8aR)-4-hydroxy-4,7-dimethyloctahydro-2H-chromen-2-yl)thiophen-2yl)benzamide
-
N-(5-((2R,4S,4aR,7R,8aS)-4-hydroxy-4,7-dimethyloctahydro-2H-chromen-2-yl)thiophen-2-yl)adamantane-1-carboxamide
-
N-(6-Aminohexyl)-5-chloro-1-naphthalenesulfonamide
-
W7, 10 microM, a calcium-calmodulin inhibitor
N-phenyl-2-(piperidin-1-yl)acetamide
-
N-phenyl-2-(pyrrolidin-1-yl)acetamide
-
N-[2-(1-[6,7-dimethoxy-2-[(E)-2-(pyridin-3-yl)ethenyl]quinazolin-4-yl]piperidin-4-yl)ethyl]sulfuric diamide
-
-
N-[2-[1-(2-ethyl-6,7-dimethoxyquinazolin-4-yl)piperidin-4-yl]ethyl]sulfuric diamide
-
-
N-[2-[1-(6,7-dimethoxyquinazolin-4-yl)piperidin-4-yl]ethyl]sulfuric diamide
-
enzyme binding, structure modelling, overview
N-[2-[1-(6-chloroquinazolin-4-yl)piperidin-4-yl]ethyl]sulfuric diamide
-
-
N-[2-[1-(7-chloroquinazolin-4-yl)piperidin-4-yl]ethyl]sulfuric diamide
-
-
N-[2-[1-(7-methoxyquinazolin-4-yl)piperidin-4-yl]ethyl]sulfuric diamide
-
-
N-[6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl]acetamide
-
-
N2,N2-dibutyl-N-[8-(trifluoromethyl)-1,2,3,4,5-benzopentathiepin-6-yl]glycinamide
-
Na3AsO4
-
slight inhibition
Naphthomycin
-
tumor cell line
neomycin B
-
a aminoglycoside
nucleoside 5'-triphosphate
-
-
nucleoside 5'monophosphate
-
-
nucleoside-5'-diphosphate
-
-
O-methyl O-(4-nitrophenyl) hydrogen phosphorothioate
-
-
o-phenanthroline
-
99% inhibition
p-chloromercuribenzoate
-
slight inhibition
p-Diazobenzenesulfonic acid
-
DASA: 84% inhibition
phenylalanine
-
5 mM, 87% residual activity
phenylmethylsulfonyl fluoride
-
FS-44: 5'-PDase activity of bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase
phosphate
-
slight inhibition
rolipram
-
a PDE 4 inhibitor
terminal 3'-monophosphoryl group of substrates
-
trequinsin
-
a PDE 3 inhibitor
vinpocetin
-
10 mU, surpresses the increase of activity, caused by the addition of 0.2 mM Ca2+
ZnSO4
-
slight inhibition
1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one
-
-
1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
1,2-dimethyl-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
-
1,2-dimethyl-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
-
1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
-
1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
-
1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10,12-dibromo-1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10,12-dibromo-1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10,12-dibromo-1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10,12-dibromo-1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10,12-dibromo-1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10,12-dibromo-1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10,12-dibromo-1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10,12-dibromo-1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10,12-dibromo-1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10,12-dibromo-1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10,12-dibromo-3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10,12-dibromo-3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10,12-dibromo-3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10,12-dibromo-3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10-bromo-1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10-bromo-1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10-bromo-1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10-bromo-1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10-bromo-1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10-bromo-1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10-bromo-1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10-bromo-1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10-bromo-1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10-bromo-1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10-bromo-3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10-bromo-3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
10-bromo-3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
10-bromo-3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
11,13-dibromo-1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one
-
-
11,13-dibromo-1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
11-bromo-1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one
-
-
11-bromo-1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
2-mercaptoethanol
-
-
2-mercaptoethanol
-
inactivation reversed by Zn2+
3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
-
3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
5'-deoxyribonucleotides
-
end-product inhibition
-
5'-deoxyribonucleotides
-
end-product inhibition
-
5'-deoxyribonucleotides
-
-
-
5'-deoxyribonucleotides
-
end-product inhibition
-
5'-nucleotides
-
end-product inhibition
5'-nucleotides
-
end-product inhibition
5'-nucleotides
-
end-product inhibition
5'-nucleotides
-
end-product inhibition
5'-ribonucleotides
-
end-product inhibition
-
5'-ribonucleotides
-
end-product inhibition
-
5-[3-benzyloxyphenyl]-1,3,4-oxadiazole-2(3H)-thione
-
-
5-[3-benzyloxyphenyl]-1,3,4-oxadiazole-2(3H)-thione
-
-
5-[4-(t-butyldimethylsilyloxy)-phenyl]-1,3,4-oxadiazole-2(3H)-thione
-
-
5-[4-(t-butyldimethylsilyloxy)-phenyl]-1,3,4-oxadiazole-2(3H)-thione
-
-
5-[4-benzyloxyphenyl]-1,3,4-oxadiazole-2(3H)-thione
-
-
5-[4-benzyloxyphenyl]-1,3,4-oxadiazole-2(3H)-thione
-
-
5-[4-hydroxyphenyl]-1,3,4-thiadiazole-2(3H)-thione
-
-
5-[4-hydroxyphenyl]-1,3,4-thiadiazole-2(3H)-thione
-
-
5-[4-pyridyl]-1,3,4-thiadiazole-2(3H)-thione
-
-
5-[4-pyridyl]-1,3,4-thiadiazole-2(3H)-thione
-
-
9,11-dibromo-1,2-dimethyl-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
-
9,11-dibromo-1,2-dimethyl-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
9,11-dibromo-1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
-
9,11-dibromo-1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
9,11-dibromo-1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
-
9,11-dibromo-1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
9,11-dibromo-1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
-
9,11-dibromo-1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
9-bromo-1,2-dimethyl-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
-
9-bromo-1,2-dimethyl-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
9-bromo-1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
-
9-bromo-1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
9-bromo-1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
-
9-bromo-1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
9-bromo-1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
-
9-bromo-1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
ADP
-
-
AMP
-
product inhibition
AMP
-
5'-AMP, competitive
AMP
-
5'-AMP, but 2'-AMP, 3'-AMP, 3': 5'cAMP and 2': 3'cAMP has no inhibiting effects; competitive; product inhibition
AMP
-
product inhibition of NPP1
AMP
-
5'-AMP and slightly 3'-AMP
AMP
-
0.5 mM, 70% residual activity
ATP
-
-
ATP
-
inhibition in decreasing order: alpha,beta-methylene-adenosine triphosphate, ATP, UTP, GTP, CTP
bis(1,3,4-oxadiazol-2-propyl)-5-thione
-
-
bis(1,3,4-oxadiazol-2-propyl)-5-thione
-
-
Co2+
-
FS-44: 5'-PDase activity of bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase
Cu2+
-
FS-44: 5'-PDase activity of bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase
CuSO4
-
-
dithiothreitol
-
-
dithiothreitol
-
inactivation reversed by Zn2+
dithiothreitol
-
liver, spleen, thymus
EDTA
-
-
EDTA
-
inactivation reversed by Mg2+, Mn2+, Ca2+, Zn2+ and slightly by Co2+
EDTA
-
91% inhibition; inactivation reversed by Zn2+
EDTA
-
inactivation reversed by Zn2+ to 90% , by Co2+ to 40% , by Ca2+ to 25%
EDTA
-
completely, inactivation reversed by Ca2+, Co2+ and, at best, with Zn2+
EDTA
-
PC-1, nucleotide pyrophosphatase/phosphodiesterase I: glycine-enhanced inhibition, reversed by Mg2+
EDTA
-
inactivation reversed by Zn2+
EDTA
-
complete inhibition, addition of EDTA plus Ca2+ or Mn2+ results in partial inhibition
EDTA
-
drastic reduction of activity
EDTA
-
high concentration
EGTA
-
-
furamidine
-
-
glutathione
-
-
glycine
-
PC-1, nucleotide pyrophosphatase/phosphodiesterase I: at high concentrations, 100 mM; PC-1, nucleotide pyrophosphatase/phosphodiesterase I: glycine-enhanced inhibition by EDTA, by itself, up to 25 mM, is not inhibitory
glycine
-
liver, 0.1 M glycine, inhibition initially 20-30%, 90% inhibition obtained after 60 min preincubation
GTP
-
competitive
GTP
-
inhibition in decreasing order: alpha,beta-methylene-adenosine triphosphate, ATP, UTP, GTP, CTP
Hg2+
-
FS-44: 5'-PDase activity of bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase
HgCl2
-
-
IBMX
-
-
IBMX
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intra peritoneal to the rats
indomethacin
-
-
indomethacin
-
PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats
L-cysteine
-
-
L-cysteine
-
inactivation reversed by Zn2+
Mn2+
-
FS-44: 5'-PDase activity of bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase
Mn2+
-
inhibition at higher concentration, 0.1-0.5 mM
N-ethylmaleimide
-
tumor cell line, N-ethylmaleimide-sensitive
N-ethylmaleimide
-
tumor cell line, N-ethylmaleimide-sensitive
N-ethylmaleimide
-
lymphoblastoma; tumor cell line, N-ethylmaleimide-sensitive
NAD+
-
competitive
NADP+
-
-
Ni2+
-
-
NSC 88915
-
a steroid inhibitor
NSC88915
a deoxycorticosterone derivative of progesterone coupled to methyl-p-toluene-sulfonate, structure-activity relationship analogues of this active compound that have a chemical substitution at a single position show a dramatic decrease in inhibition activity
NSC88915
-
a steroid inhibitor
Reducing agents
-
-
-
Reducing agents
-
inactivation reversed by Zn2+
-
suramin
-
0.25 mM, inhibition
suramin
-
0.25 mM, 87% residual activity
suramin
-
0.25 mM, about 46% inhibition
terminal 3'-monophosphoryl group of substrates
-
-
-
terminal 3'-monophosphoryl group of substrates
-
-
-
terminal 3'-monophosphoryl group of substrates
-
-
-
terminal 3'-monophosphoryl group of substrates
-
-
-
terminal 3'-monophosphoryl group of substrates
-
-
-
UMP
-
-
UMP
-
5'-UMP and very slightly 3'-UMP
UTP
-
inhibition in decreasing order: alpha,beta-methylene-adenosine triphosphate, ATP, UTP, GTP, CTP
vinpocetine
-
-
vinpocetine
-
40 microM, selective PDE1 inhibitor
vinpocetine
-
a PDE 1 inhibitor
Zn2+
-
FS-44: 5'-PDase activity of bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase
Zn2+
-
tumor cell line, N-ethylmaleimide-sensitive
Zn2+
-
tumor cell line, N-ethylmaleimide-sensitive
Zn2+
-
lymphoblastoma; tumor cell line, N-ethylmaleimide-sensitive
additional information
-
no inhibition by anions
-
additional information
-
the enzyme is not inhibited by 5-[4-pyridyl]-1,3,4-oxadiazole-2(3H)-thione, 5-[3-benzyloxyphenyl]-1,3,4-oxadiazole-2(3H)-thione, 5-[4-benzyloxyphenyl]-3-octyl-1,3,4-oxadiazole-2(3H)-thione, 5-[4-benzyloxyphenyl]-3-benzyl-1,3,4-oxadiazole-2(3H)-thione, 5-[4-benzyloxyphenyl]-3-pentyl-1,3,4-oxadiazole-2(3H)-thione, 5-cyclohexyl-1,3,4-oxadiazole-2(3H)-thione, 5-diphenylmethyl-1,3,4-oxadiazole-2(3H)-thione, 5-[4-benzyloxyphenyl]-3-benzoyl-1,3,4-oxadiazole-2(3H)-thione, 5-[4-benzyloxyphenyl]-3-(2-hydroxyethyl)-1,3,4-oxadiazole-2(3H)-thione, 5-[1-naphthyl]-1,3,4-oxadiazole-2(3H)-thione, 5-phenyl-1,3,4-thiadiazole-2(3H)-thione, 5-[4-hydroxyphenyl]-3-benzyl-1,3,4-thiadiazole-2(3H)-thione, 5-[4-propoxyphenyl]-3-propyl-1,3,4-thiadiazole-2(3H)-thione, 5-diphenylmethyl-1,3,4-thiadiazole-2(3H)-thionr, 5-[4-hydroxyphenyl]-1,3,4-thiadiazole-2(3H)-thione, and 5-[4-benzyloxyphenyl]-3-benzyl-1,3,4-thiaadiazole-2(3H)-thione
-
additional information
-
no inhibition by adenosine, inosine, phenylalanine and caffeine
-
additional information
-
no inhibition by L-ascorbic acid
-
additional information
-
not inhibitory: 3-isobutyl-1methylxanthine, Ro 20-1724, 13-dipropyl-8-p-sulfophenylxanthine
-
additional information
-
expression of PC-1 is down-regulated during adipocyte maturation
-
additional information
-
the enzyme is not inhibited by bis(1,3,4-oxadiazol-2-methyl)-5-thione, 5-[4-pyridyl]-1,3,4-oxadiazole-2(3H)-thione, 5-[3-hydroxyphenyl]-1,3,4-oxadiazole-2(3H)-thione, 5-[4-benzyloxyphenyl]-3-octyl-1,3,4-oxadiazole-2(3H)-thione, and 5-[4-(t-butyldimethylsilyloxy)-phenyl]-1,3,4-thiadiazole-2 (3H)-thione
-
additional information
-
design, synthesis, and evaluation of new indenoisoquinolines that are dual inhibitors of both tyrosyl-DNA phosphodiesterase I and topoisomerase 1, structure-activity relationships and cytotoxicity, overview. No inhibition by methyl 2-[(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-2-oxoacetate, methyl 3-[(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-3-oxopropanoate, methyl 4-[(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-4-oxobutanoate, methyl 5-[(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-5-oxopentanoate, methyl 6-[(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-6-oxohexanoate, 3-[(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]-isoquinolin-3-yl)amino]-3-oxopropanoic acid, methyl 3-[(6-(3-((tert-butoxycarbonyl)amino)propyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl)amino]-3-oxopropanoate, methyl 4-[(6-(3-((tert-butoxycarbonyl)amino)propyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl)amino]-4-oxobutanoate, methyl 5-[(6-(3-((tert-butoxycarbonyl)amino)propyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl)amino]-5-oxopentanoate, 5-[(6-(3-((tert-butoxycarbonyl)amino)propyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl)amino]-5-oxopentanoic acid, 2-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-2-oxoacetic acid, 3-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-3-oxopropanoic acid, 4-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-4-oxobutanoic acid, 5-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-5-oxopentanoic acid, 6-[(6-(3-aminopropyl)-5,11-dioxo-6,11-dihydro-5H-indeno-[1,2-c]isoquinolin-3-yl)amino]-6-oxohexanoic acid, ethyl 2-[(6-Methyl-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl)amino]acetate, 2-[(6-methyl-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]-isoquinolin-3-yl)amino]acetic acid, 2-((6-(3-((tert-butoxycarbonyl)amino)propyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl)amino)acetic acid, 6-(3-bromopropyl)-5,6-dihydro-8-methoxy-3-nitro-5,11-dioxo-11H-indeno[1,2-c]isoquinoline, 6-(3-azidopropyl)-5,6-dihydro-8-methoxy-3-nitro-5,11-dioxo-11H-indeno[1,2-c]isoquinoline, 8-methoxy-6-(3-morpholinopropyl)-3-nitro-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione, N-[5,11-dioxo-6-[3-(2l5-triaz-1-en-2-yn-1-yl)propyl]-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl]acetamide, N-[6-(3-hydroxypropyl)-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl]acetamide, N-[6-(3-aminopropyl)-11-hydroxy-5-oxo-6,11-dihydro-5H-indeno[1,2-c]isoquinolin-3-yl]acetamide, 6-(3-hydroxypropyl)-3-nitro-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione, 3-cyano-5,11-dihydro-6-[3-(1H-imidazolyl)propyl]-5,11-dioxo-6,11-dihydro-5H-indeno[1,2-c]isoquinoline, 3-cyano-6,11-dihydro-5,11-dioxo-6-(3-morpholinylpropyl)-5H-indeno[1,2-c]isoquinoline, and 3-cyano-5,11-dihydro-6-[3-(dimethylamino)propyl]-5,11-dioxoindeno[1,2-c]isquinoline. Molecular modeling of the enzyme based on crystal structure PDB 1RFF
-
additional information
docking simulations suggest that enzyme inhibitors bind within the catalytic pocket to prevent docking of endogenous substrates
-
additional information
-
synthesis and evaluation of dual tyrosyl-DNA phosphodiesterase I-topoisomerase I inhibitors based on the indenoisoquinoline chemotype, structure-activity relationship studies, overview
-
additional information
-
structure-based drug design, synthesis, and biological evaluation of O-2-modified indenoisoquinolines as dual topoisomerase I-tyrosyl-DNA phosphodiesterase I inhibitors, structure-activity relationships, molecular docking studies, and molecular modeling, overview. No inhibition by 2-(allyloxy)-3-methoxy-6-(3-morpholinopropyl)-5H-[1,3]-dioxolo[4',5':5,6]indeno [1,2-c]isoquinoline-5,12(6H)-dione, 3-methoxy-2-(3-morpholinopropoxy)-6-(3-morpholinopropyl)-5H-[1,3]dioxolo[4',5':5,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione, 3-methoxy-2-(3-(4-methylpiperazin-1-yl)propoxy)-6-(3-morpholinopropyl)-5H-[1,3]dioxolo[4',5':5,6]indeno[1,2-c]-isoquinoline-5,12(6H)-dione, methyl 2-((3-methoxy-6-(3-morpholinopropyl)-5,12-dioxo-6,12-dihydro-5H-[1,3]dioxolo[4',5':5,6]indeno[1,2-c]-isoquinolin-2-yl)oxy)acetate, and 2-((12-hydroxy-3-methoxy-6-(3-morpholinopropyl)-5-oxo-6,12-dihydro-5H-[1,3]dioxolo[4',5':5,6]indeno[1,2-c]-isoquinolin-2-yl)oxy)acetohydrazide. Antiproliferative potencies of selected O-2-modified indenoisoquinolines, overview
-
additional information
-
design and synthesis of highly potent and selective ectonucleotide pyrophosphatase/phosphodiesterase I inhibitors based on an adenosine 5-(alpha or gamma)-thio-(alpha,beta- or beta,gamma)-methylenetriphosphate scaffold, compound configurations analsis by NMR spectroscopy, overview. Analogue 4 is not a good inhibitor. The thiophosphate groups are designed to chelate the tentative Zn2+ ions. Docking od 1-3 into the NPP1 model suggests that activity correlates with the number of H-bonds with binding site residues, overview
-
additional information
-
no inhibition by divalent cations, Mg2+ and Ca2+ , or p-chloromercuribenzoate
-
additional information
PC-1 promoter activity induced by osteoblast differentiation is inhibited by fibroblast growth factor 2
-
additional information
-
PC-1, no inhibition by MgCl2 and /or CaCl2
-
additional information
-
not inhibitory: ouabain, N-ethylmaleimide, levamisole, sodium azide
-
additional information
-
not inhibitory to renal ecto-phosphodiesterase: 8-methoxymethyl-3-isobutyl-1-methylxanthine, erythro-9-(2-hydroxy-3-nonyl)adenine, milrinone, cGMP, 4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one, zaprinast, 5-nitro-2,N,N-trimethylbenzenesulfonamide
-
additional information
-
not inhibitory: levamisole, sodium azide, gadolinium chloride
-
additional information
-
synthesis of 1,2,9,11-tetrasubstituted 7H-thieno[2',3':4,5]pyrimido[6,1-b]-quinazolin-7-one and 1,3,10,12-tetrasubstituted 8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one inhibitors, synthesis and evaluation, overview
-
additional information
-
bicarbonate acts synergistically with inhibitor IC86340
-
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0.0011 - 0.0048
(5'-GATCTAAAAGACTT-3')-phosphotyrosine
83
2-naphthyl chloromethylphosphonate
-
-
120
2-naphthyl methylphosphonate
-
-
18
2-naphthyl phenylphosphonate
-
-
0.26
3'-O-acetyl-p-nitrophenylthymidine 5'-phosphate
-
pH 8.0
4.9 - 8.2
4-methylumbelliferyl phenylphosphonate
0.22 - 2
4-methylumbelliferyl thymidine 5'-phosphate
0.09
4-nitrophenyl deoxythymidine 5'-phosphat
-
-
-
0.19 - 0.41
4-nitrophenyl uridine 5'-phosphate
-
0.96
5'-p-nitrophenyladenosine 5'-phosphate
-
FS-44: 5'-PDase activity of bifunctional enzyme: cyclic-ribonucleotide phosphomutase-5'-phosphodiesterase
0.8
bis(4-methylumbelliferyl) phosphate
-
-
1.2 - 22.2
bis(4-nitrophenyl)phosphate
0.25 - 14.4
bis(p-nitrophenyl) phosphate
0.15 - 18.3
bis-p-nitrophenyl phosphate
0.001 - 0.011
diadenosine 5',5'''-P1,P3-triphosphate
0.0006 - 0.008
diadenosine 5',5'''-P1,P4-tetraphosphate
0.012
diguanosine 5',5'''-P1,P4-tetraphosphate
-
-
0.022
diuridine tetraphosphate
-
pH 7.4, 37°C
0.035 - 0.281
p-nitrophenyl 5'-thymidine monophosphate
41
p-nitrophenyl chloromethylphosphonate
-
-
1.7 - 73
p-nitrophenyl ethyl phosphate
66
p-nitrophenyl methylphosphonate
-
-
0.31 - 202
p-Nitrophenyl phenylphosphonate
1.53 - 3.33
p-Nitrophenylphosphorylcholine
0.043 - 6
p-nitrophenylthymidine 5'-phosphate
0.097 - 0.22
thymidine 5'-monophosphate p-nitrophenylester
additional information
additional information
-
kinetics of enzyme cleavage activity on different apurinic/apyrimidinic-DNA substrates., overview
-
0.0011
(5'-GATCTAAAAGACTT-3')-phosphotyrosine
wild type enzyme, at pH 7.5 and 30°C
0.0026
(5'-GATCTAAAAGACTT-3')-phosphotyrosine
mutant enzyme H432N, at pH 7.5 and 30°C
0.0034
(5'-GATCTAAAAGACTT-3')-phosphotyrosine
mutant enzyme H182A, at pH 7.5 and 30°C
0.0048
(5'-GATCTAAAAGACTT-3')-phosphotyrosine
mutant enzyme H432R, at pH 7.5 and 30°C
4.9
4-methylumbelliferyl phenylphosphonate
-
-
8.2
4-methylumbelliferyl phenylphosphonate
-
-
0.22
4-methylumbelliferyl thymidine 5'-phosphate
-
-
2
4-methylumbelliferyl thymidine 5'-phosphate
-
-
0.19
4-nitrophenyl uridine 5'-phosphate
-
-
-
0.41
4-nitrophenyl uridine 5'-phosphate
-
-
-
1.2
bis(4-nitrophenyl)phosphate
-
mutant P178A, pH 7.4, 37°C
1.8
bis(4-nitrophenyl)phosphate
-
mutant R252G, pH 7.4, 37°C
3.5
bis(4-nitrophenyl)phosphate
-
mutant E208A, pH 7.4, 37°C
6
bis(4-nitrophenyl)phosphate
-
mutant C40G, pH 7.4, 37°C
6.5
bis(4-nitrophenyl)phosphate
-
mutant F51L, pH 7.4, 37°C
8
bis(4-nitrophenyl)phosphate
-
mutant G62V, pH 7.4, 37°C
8.5
bis(4-nitrophenyl)phosphate
-
wild-type, pH 7.4, 37°C
13.2
bis(4-nitrophenyl)phosphate
-
mutant C25G, pH 7.4, 37°C
22.2
bis(4-nitrophenyl)phosphate
-
mutant P64A, pH 7.4, 37°C
0.25
bis(p-nitrophenyl) phosphate
-
-
0.85
bis(p-nitrophenyl) phosphate
-
-
1.6
bis(p-nitrophenyl) phosphate
-
-
2.7
bis(p-nitrophenyl) phosphate
-
-
8
bis(p-nitrophenyl) phosphate
-
milk fat globule membrane
14.4
bis(p-nitrophenyl) phosphate
-
cytoplasmic membrane of mammary gland
0.15
bis-p-nitrophenyl phosphate
+/- 0.01, with 1 mM Ni2+
0.33
bis-p-nitrophenyl phosphate
-
pH 5.0, 60°C
0.66
bis-p-nitrophenyl phosphate
+/- 0.09, with 20 mM PO43- and 1 mM Ni2+
1.01
bis-p-nitrophenyl phosphate
+/- 0.13, with 50 mM PO43- and 1 mM Ni2+
9.74
bis-p-nitrophenyl phosphate
-
pH 8.5, 37°C
18.3
bis-p-nitrophenyl phosphate
-
pH 8.5, 37°C, presence of 0.5 mM phosphate
0.001
diadenosine 5',5'''-P1,P3-triphosphate
-
Ap3A
0.0022
diadenosine 5',5'''-P1,P3-triphosphate
-
-
0.011
diadenosine 5',5'''-P1,P3-triphosphate
-
-
0.0006
diadenosine 5',5'''-P1,P4-tetraphosphate
-
Ap4A
0.002
diadenosine 5',5'''-P1,P4-tetraphosphate
-
-
0.008
diadenosine 5',5'''-P1,P4-tetraphosphate
-
-
0.0096
NAD+
-
-
0.035
p-nitrophenyl 5'-thymidine monophosphate
+/- 0.003, with 1 mM Ni2+
0.106
p-nitrophenyl 5'-thymidine monophosphate
-
pH 8.9, 37°C
0.281
p-nitrophenyl 5'-thymidine monophosphate
-
pH 7.4, 37°C
1.7
p-nitrophenyl ethyl phosphate
-
mutant enzyme C57S, at 30°C, in 44 mM succinic acid, 33 mM imidazole, 33 mM diethanolamine, pH 7.5
2.3
p-nitrophenyl ethyl phosphate
-
wild type enzyme, at 30°C, in 44 mM succinic acid, 33 mM imidazole, 33 mM diethanolamine, pH 7.5
2.9
p-nitrophenyl ethyl phosphate
-
mutant enzyme C57A, at 30°C, in 44 mM succinic acid, 33 mM imidazole, 33 mM diethanolamine, pH 7.5
4.8
p-nitrophenyl ethyl phosphate
-
mutant enzyme T107A, at 30°C, in 44 mM succinic acid, 33 mM imidazole, 33 mM diethanolamine, pH 7.5
45
p-nitrophenyl ethyl phosphate
-
mutant enzyme N78A, at 30°C, in 44 mM succinic acid, 33 mM imidazole, 33 mM diethanolamine, pH 7.5
50
p-nitrophenyl ethyl phosphate
-
mutant enzyme Q13A, at 30°C, in 44 mM succinic acid, 33 mM imidazole, 33 mM diethanolamine, pH 7.5
57
p-nitrophenyl ethyl phosphate
-
mutant enzyme H218A, at 30°C, in 44 mM succinic acid, 33 mM imidazole, 33 mM diethanolamine, pH 7.5
70
p-nitrophenyl ethyl phosphate
-
Km above 70 mM, mutant enzyme Y105A, at 30°C, in 44 mM succinic acid, 33 mM imidazole, 33 mM diethanolamine, pH 7.5
73
p-nitrophenyl ethyl phosphate
-
mutant enzyme K337A, at 30°C, in 44 mM succinic acid, 33 mM imidazole, 33 mM diethanolamine, pH 7.5
0.31
p-Nitrophenyl phenylphosphonate
-
mutant enzyme T107A, at 30°C, in 44 mM succinic acid, 33 mM imidazole, 33 mM diethanolamine, pH 7.5
2.8
p-Nitrophenyl phenylphosphonate
-
mutant enzyme C57A, at 30°C, in 44 mM succinic acid, 33 mM imidazole, 33 mM diethanolamine, pH 7.5
3
p-Nitrophenyl phenylphosphonate
-
wild type enzyme, at 30°C, in 44 mM succinic acid, 33 mM imidazole, 33 mM diethanolamine, pH 7.5
3.8
p-Nitrophenyl phenylphosphonate
-
mutant enzyme C57S, at 30°C, in 44 mM succinic acid, 33 mM imidazole, 33 mM diethanolamine, pH 7.5
4
p-Nitrophenyl phenylphosphonate
-
mutant enzyme N78A, at 30°C, in 44 mM succinic acid, 33 mM imidazole, 33 mM diethanolamine, pH 7.5
11
p-Nitrophenyl phenylphosphonate
-
-
14
p-Nitrophenyl phenylphosphonate
-
mutant enzyme K337A, at 30°C, in 44 mM succinic acid, 33 mM imidazole, 33 mM diethanolamine, pH 7.5
15
p-Nitrophenyl phenylphosphonate
-
-
15
p-Nitrophenyl phenylphosphonate
-
mutant enzyme H218A, at 30°C, in 44 mM succinic acid, 33 mM imidazole, 33 mM diethanolamine, pH 7.5
28
p-Nitrophenyl phenylphosphonate
-
mutant enzyme Y105A, at 30°C, in 44 mM succinic acid, 33 mM imidazole, 33 mM diethanolamine, pH 7.5
34.6
p-Nitrophenyl phenylphosphonate
-
-
43
p-Nitrophenyl phenylphosphonate
-
mutant enzyme Q13A, at 30°C, in 44 mM succinic acid, 33 mM imidazole, 33 mM diethanolamine, pH 7.5
152.2
p-Nitrophenyl phenylphosphonate
-
cytoplasmic membrane of mammary gland
202
p-Nitrophenyl phenylphosphonate
-
milk fat globule membrane
1.53
p-Nitrophenylphosphorylcholine
+/- 0.1, with 20 mM Mn2+
3.33
p-Nitrophenylphosphorylcholine
+/- 0.5, with 1 mM Ni2+
0.043
p-nitrophenylthymidine 5'-phosphate
-
-
0.046
p-nitrophenylthymidine 5'-phosphate
-
pH 9.1
0.068
p-nitrophenylthymidine 5'-phosphate
-
liver of DBA/2 mice
0.091
p-nitrophenylthymidine 5'-phosphate
-
pH 8.9, 37°C
0.17
p-nitrophenylthymidine 5'-phosphate
-
pH 8.0
0.2
p-nitrophenylthymidine 5'-phosphate
-
-
0.28
p-nitrophenylthymidine 5'-phosphate
-
-
0.4
p-nitrophenylthymidine 5'-phosphate
-
-
0.41
p-nitrophenylthymidine 5'-phosphate
-
-
0.7
p-nitrophenylthymidine 5'-phosphate
-
-
1.54
p-nitrophenylthymidine 5'-phosphate
-
lymphoblastoma L5178Y
1.6
p-nitrophenylthymidine 5'-phosphate
-
milk fat globule membrane
1.7
p-nitrophenylthymidine 5'-phosphate
-
cytoplasmic membrane of mammary gland
6
p-nitrophenylthymidine 5'-phosphate
-
-
0.097
thymidine 5'-monophosphate p-nitrophenylester
-
pH 9.6, gp115, AS30D protein
0.22
thymidine 5'-monophosphate p-nitrophenylester
-
pH 9.6, gp120/gp110, liver protein
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0.015
(2R,4R,4aR,7R,8aS)-4,7-dimethyl-2-(5-aminothiophen-2-yl)octahydro-2H-chromen-4-ol
Homo sapiens
at pH 8.0 and 26°C
0.015
(2R,4S,4aR,7R,8aS)-4,7-dimethyl-2-(5-aminothiophen-2-yl)octahydro-2H-chromen-4-ol
Homo sapiens
at pH 8.0 and 26°C
0.0006
(RP)-adenosine 5'-(alpha-thio-beta,gamma-dichloromethylene)triphosphate
Homo sapiens
-
pH 8.5, 37°C, enzyme NPP1
0.0163
(RP)-adenosine 5'-(alpha-thio-beta,gamma-methylene)triphosphate
Homo sapiens
-
pH 8.5, 37°C, enzyme NPP1
0.0312
(SP)-adenosine 5'-(alpha-thio-beta,gamma-dichloromethylene)triphosphate
Homo sapiens
-
pH 8.5, 37°C, enzyme NPP1
0.0187
(SP)-adenosine 5'-(alpha-thio-beta,gamma-methylene)triphosphate
Homo sapiens
-
pH 8.5, 37°C, enzyme NPP1
0.23
1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.3
1,2-dimethyl-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.08
1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.1
1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.12
1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.07
1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.07
1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.09
1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.23
1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.06
1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.07
10,12-dibromo-1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.06
10,12-dibromo-1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.03
10,12-dibromo-1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.05
10,12-dibromo-1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.07
10,12-dibromo-1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.08
10,12-dibromo-3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.07
10,12-dibromo-3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.1
10-bromo-1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.07
10-bromo-1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.08
10-bromo-1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.08
10-bromo-1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.07
10-bromo-1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.1
10-bromo-3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.1
10-bromo-3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.1
11,13-dibromo-1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.13
11-bromo-1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.004
2,2,2-trifluoro-N-(5-((2R,4R,4aR,7R,8aR)-4-hydroxy-4,7-dimethyloctahydro-2H-chromen-2-yl)thiophen-2-yl)acetamide
Homo sapiens
at pH 8.0 and 26°C
0.0014
2,2,2-trifluoro-N-(5-((2R,4S,4aR,7R,8aR)-4-hydroxy-4,7-dimethyloctahydro-2H-chromen-2-yl)thiophen-2-yl)acetamide
Homo sapiens
at pH 8.0 and 26°C
0.01
2,2,2-trifluoro-N-(8-(trifluoromethyl)benzo[f][1,2,3,4,5]pentathiepin-6-yl)acetamide
Homo sapiens
IC50 above 0.1 mM, at pH 8.0 and 26°C
0.00022
2-(dibutylamino)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide
Homo sapiens
at pH 8.0 and 26°C
0.00128
2-(piperidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide
Homo sapiens
at pH 8.0 and 26°C
0.0037
2-(pyrrolidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide
Homo sapiens
at pH 8.0 and 26°C
0.00162
2-morpholino-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)acetamide
Homo sapiens
at pH 8.0 and 26°C
0.00123
3-(((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one
Homo sapiens
pH and temperature not specified in the publication
0.0012
3-(((1S,5R)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one
Homo sapiens
pH and temperature not specified in the publication
0.01
3-((3,4,5-trimethoxybenzyl)oxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one
Homo sapiens
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.00493
3-((3-methoxybenzyl)oxy)-7,8,9,10-tetrahydro-6Hbenzo[c]chromen-6-one
Homo sapiens
pH and temperature not specified in the publication
0.00145
3-(2-((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)ethoxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one
Homo sapiens
pH and temperature not specified in the publication
0.08
3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.0399
3-(4-methoxy-phenyl)-1-(3-nitro-phenyl)-8Hpyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
Rattus norvegicus
-
-
0.04
3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.00562
3-(benzyloxy)-7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one
Homo sapiens
pH and temperature not specified in the publication
0.00366
3-(piperidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)propanamide
Homo sapiens
at pH 8.0 and 26°C
0.00603
3-(pyrrolidin-1-yl)-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)propanamide
Homo sapiens
at pH 8.0 and 26°C
0.0013
3-morpholino-N-(8-(trifluoromethyl)benzo[f]-[1,2,3,4,5]pentathiepin-6-yl)propanamide
Homo sapiens
at pH 8.0 and 26°C
0.01
4-methyl-7-((3,4,5-trimethoxybenzyl)oxy)-2H-chromen-2-one
Homo sapiens
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.494
5-[3-benzyloxyphenyl]-1,3,4-oxadiazole-2(3H)-thione
Homo sapiens
-
in 20 mM Tris-HCl, pH 8.0, 0.5 M NaCl and 1 mM CaCl2, at 37°C
1
5-[3-hydroxyphenyl]-1,3,4-oxadiazole-2(3H)-thione
Bothrops atrox
-
in Tris-HCl buffer 33 mM pH 8.8, at 37°C
0.368
5-[4-(t-butyldimethylsilyloxy)-phenyl]-1,3,4-oxadiazole-2(3H)-thione
0.06647
5-[4-(t-butyldimethylsilyloxy)-phenyl]-1,3,4-thiadiazole-2(3H)-thione
Bothrops atrox
-
in Tris-HCl buffer 33 mM pH 8.8, at 37°C
0.628 - 0.9
5-[4-benzyloxyphenyl]-1,3,4-oxadiazole-2(3H)-thione
0.96
5-[4-hydroxyphenyl]-1,3,4-oxadiazole-2(3H)-thione
Bothrops atrox
-
in Tris-HCl buffer 33 mM pH 8.8, at 37°C
0.39 - 0.9
5-[4-hydroxyphenyl]-1,3,4-thiadiazole-2(3H)-thione
0.66 - 0.998
5-[4-pyridyl]-1,3,4-thiadiazole-2(3H)-thione
0.001
6,6'-[(1R,2R,3S,4S)-2,4-bis(4-hydroxyphenyl)cyclobutane-1,3-diyl]di(2H-pyran-2-one)
Homo sapiens
at pH 8.0 and 26°C
0.00152
6,6'-[propane-1,3-diylbis(iminopropane-3,1-diyl)]bis(5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione)
Homo sapiens
-
pH 7.5, 25°C, recombinant enzyme
0.014
6-(10-aminodecyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
Homo sapiens
-
pH 7.5, 25°C, recombinant enzyme
0.0128
6-(11-aminoundecyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
Homo sapiens
-
pH 7.5, 25°C, recombinant enzyme
0.0151
6-(12-aminododecyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
Homo sapiens
-
pH 7.5, 25°C, recombinant enzyme
0.0553
6-(2-aminoethyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
Homo sapiens
-
pH 7.5, 25°C, recombinant enzyme
0.0295
6-(3-aminopropyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
Homo sapiens
-
pH 7.5, 25°C, recombinant enzyme
0.0223
6-(4-aminobutyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
Homo sapiens
-
pH 7.5, 25°C, recombinant enzyme
0.0175
6-(5-aminopentyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
Homo sapiens
-
pH 7.5, 25°C, recombinant enzyme
0.025
6-(6-aminohexyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
Homo sapiens
-
pH 7.5, 25°C, recombinant enzyme
0.0288
6-(7-aminoheptyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
Homo sapiens
-
pH 7.5, 25°C, recombinant enzyme
0.048
6-(8-aminooctyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
Homo sapiens
-
pH 7.5, 25°C, recombinant enzyme
0.047
6-(9-aminononyl)-5H-indeno[1,2-c]isoquinoline-5,11(6H)-dione
Homo sapiens
-
pH 7.5, 25°C, recombinant enzyme
0.00137
7-(((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
Homo sapiens
pH and temperature not specified in the publication
0.00156
7-(((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-4-methyl-2H-chromen-2-one
Homo sapiens
pH and temperature not specified in the publication
0.000675
7-(((1S,5R)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
Homo sapiens
pH and temperature not specified in the publication
0.00431
7-(((1S,5R)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)methoxy)-4-methyl-2H-chromen-2-one
Homo sapiens
pH and temperature not specified in the publication
0.01
7-((3,4,5-trimethoxybenzyl)oxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
Homo sapiens
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.01
7-((3-methoxybenzyl) oxy)-4-methyl-2H-chromen-2-one
Homo sapiens
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.01
7-((3-methoxybenzyl)oxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
Homo sapiens
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.00109
7-(2-((1R,5S)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)ethoxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
Homo sapiens
pH and temperature not specified in the publication
0.00917
7-(benzyloxy)-2,3-dihydrocyclopenta[c]chromen-4(1H)-one
Homo sapiens
pH and temperature not specified in the publication
0.00528
7-(benzyloxy)-4-methyl-2H-chromen-2-one
Homo sapiens
pH and temperature not specified in the publication
0.0000675
7-[[(1S,5R)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl]methoxy]-2,3-dihydrobenzo[b]cyclopenta[d]pyran-4(1H)-one
Homo sapiens
at pH 8.0 and 26°C
0.1
9,11-dibromo-1,2-dimethyl-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.08
9,11-dibromo-1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.337
9,11-dibromo-1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one
Rattus norvegicus
-
-
0.06
9,11-dibromo-1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.06
9,11-dibromo-1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.15
9-bromo-1,2-dimethyl-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.09
9-bromo-1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.08
9-bromo-1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.09
9-bromo-1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.00039
adenosine 5'-(gamma-thio-beta,gamma-methylene)triphosphate
Homo sapiens
-
pH 8.5, 37°C, enzyme NPP1
0.01
aminobenzopentathiepine
Homo sapiens
IC50 above 0.01 mM, at pH 8.0 and 26°C
0.85
bis(1,3,4-oxadiazol-2-methyl)-5-thione
Bothrops atrox
-
in Tris-HCl buffer 33 mM pH 8.8, at 37°C
0.429 - 0.467
bis(1,3,4-oxadiazol-2-propyl)-5-thione
0.839
bis(1,3,4-thiadiazole-2-methyl)-5-thione
Bothrops atrox
-
in Tris-HCl buffer 33 mM pH 8.8, at 37°C
0.274
EDTA
Bothrops atrox
-
in Tris-HCl buffer 33 mM pH 8.8, at 37°C
0.0012
furamidine
Homo sapiens
at pH 8.0 and 26°C
0.02
IBMX
Bos taurus
-
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication
0.748
L-cysteine
Bothrops atrox
-
in Tris-HCl buffer 33 mM pH 8.8, at 37°C
0.0004
methyl-3,4-dephostatin
Homo sapiens
pH and temperature not specified in the publication
0.00245
N-(2-[1-[2-(2-methyl-1H-imidazol-1-yl)pyrimidin-4-yl]piperidin-4-yl]ethyl)sulfuric diamide
Homo sapiens
-
-
0.0006
N-(2-[1-[6-(2-methyl-1H-imidazol-1-yl)pyrimidin-4-yl]piperidin-4-yl]ethyl)sulfuric diamide
Homo sapiens
-
-
0.0035
N-(3,7-dimethyloct-6-en-1-yl)tricyclo[3.3.1.1(3,7)]decan-2-amine
Homo sapiens
at pH 8.0 and 26°C
0.0029
N-(5-((2R,4R,4aR,7R,8aR)-4-hydroxy-4,7-dimethyloctahydro-2H-chromen-2-yl)thiophen-2-yl)acetamide
Homo sapiens
at pH 8.0 and 26°C
0.0033
N-(5-((2R,4R,4aR,7R,8aR)-4-hydroxy-4,7-dimethyloctahydro-2H-chromen-2-yl)thiophen-2-yl)benzamide
Homo sapiens
at pH 8.0 and 26°C
0.0028
N-(5-((2R,4R,4aR,7R,8aS)-4-hydroxy-4,7-dimethyloctahydro-2H-chromen-2-yl)thiophen-2-yl)adamantane-1-carboxamide
Homo sapiens
at pH 8.0 and 26°C
0.0058
N-(5-((2R,4S,4aR,7R,8aR)-4-hydroxy-4,7-dimethyloctahydro-2H-chromen-2-yl)thiophen-2-yl)acetamide
Homo sapiens
at pH 8.0 and 26°C
0.005
N-(5-((2R,4S,4aR,7R,8aR)-4-hydroxy-4,7-dimethyloctahydro-2H-chromen-2-yl)thiophen-2yl)benzamide
Homo sapiens
at pH 8.0 and 26°C
0.00124
N-(5-((2R,4S,4aR,7R,8aS)-4-hydroxy-4,7-dimethyloctahydro-2H-chromen-2-yl)thiophen-2-yl)adamantane-1-carboxamide
Homo sapiens
at pH 8.0 and 26°C
0.01
N-phenyl-2-(piperidin-1-yl)acetamide
Homo sapiens
IC50 above 0.1 mM, at pH 8.0 and 26°C
0.01
N-phenyl-2-(pyrrolidin-1-yl)acetamide
Homo sapiens
IC50 above 0.1 mM, at pH 8.0 and 26°C
0.000035
N-[2-(1-[6,7-dimethoxy-2-[(E)-2-(pyridin-3-yl)ethenyl]quinazolin-4-yl]piperidin-4-yl)ethyl]sulfuric diamide
Homo sapiens
-
-
0.000214
N-[2-[1-(2-ethyl-6,7-dimethoxyquinazolin-4-yl)piperidin-4-yl]ethyl]sulfuric diamide
Homo sapiens
-
-
0.000036
N-[2-[1-(6,7-dimethoxyquinazolin-4-yl)piperidin-4-yl]ethyl]sulfuric diamide
Homo sapiens
-
-
0.00598
N-[2-[1-(6-chloroquinazolin-4-yl)piperidin-4-yl]ethyl]sulfuric diamide
Homo sapiens
-
-
0.01
N-[2-[1-(7-chloroquinazolin-4-yl)piperidin-4-yl]ethyl]sulfuric diamide
Homo sapiens
-
above
0.000187
N-[2-[1-(7-methoxyquinazolin-4-yl)piperidin-4-yl]ethyl]sulfuric diamide
Homo sapiens
-
-
0.009
NSC88915
Homo sapiens
pH and temperature not specified in the publication
additional information
indomethacin
Bos taurus
-
not tested
0.368
5-[4-(t-butyldimethylsilyloxy)-phenyl]-1,3,4-oxadiazole-2(3H)-thione
Homo sapiens
-
in 20 mM Tris-HCl, pH 8.0, 0.5 M NaCl and 1 mM CaCl2, at 37°C
0.368
5-[4-(t-butyldimethylsilyloxy)-phenyl]-1,3,4-oxadiazole-2(3H)-thione
Bothrops atrox
-
in Tris-HCl buffer 33 mM pH 8.8, at 37°C
0.628
5-[4-benzyloxyphenyl]-1,3,4-oxadiazole-2(3H)-thione
Homo sapiens
-
in 20 mM Tris-HCl, pH 8.0, 0.5 M NaCl and 1 mM CaCl2, at 37°C
0.9
5-[4-benzyloxyphenyl]-1,3,4-oxadiazole-2(3H)-thione
Bothrops atrox
-
in Tris-HCl buffer 33 mM pH 8.8, at 37°C
0.39
5-[4-hydroxyphenyl]-1,3,4-thiadiazole-2(3H)-thione
Bothrops atrox
-
in Tris-HCl buffer 33 mM pH 8.8, at 37°C
0.9
5-[4-hydroxyphenyl]-1,3,4-thiadiazole-2(3H)-thione
Homo sapiens
-
in 20 mM Tris-HCl, pH 8.0, 0.5 M NaCl and 1 mM CaCl2, at 37°C
0.66
5-[4-pyridyl]-1,3,4-thiadiazole-2(3H)-thione
Bothrops atrox
-
in Tris-HCl buffer 33 mM pH 8.8, at 37°C
0.998
5-[4-pyridyl]-1,3,4-thiadiazole-2(3H)-thione
Homo sapiens
-
in 20 mM Tris-HCl, pH 8.0, 0.5 M NaCl and 1 mM CaCl2, at 37°C
0.429
bis(1,3,4-oxadiazol-2-propyl)-5-thione
Bothrops atrox
-
in Tris-HCl buffer 33 mM pH 8.8, at 37°C
0.467
bis(1,3,4-oxadiazol-2-propyl)-5-thione
Homo sapiens
-
in 20 mM Tris-HCl, pH 8.0, 0.5 M NaCl and 1 mM CaCl2, at 37°C
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evolution
conservation of the active site motifs typical for all Tdp1 proteins
evolution
the enzyme belongs to the phospholipase D, PLD, superfamily, which consists of a highly diverse collection of prokaryotic and eukaryotic enzymes, such as bacterial, plant and mammalian PLDs, cardiolipin and phosphatidylserine synthases, Salmonella typhimurium Nuc and mammalian DNase II endonucleases, restriction enzyme BfiI, poxvirus envelope proteins p37K and K4L, and eukaryotic Tdp1, sequence comparison. Family members show the presence of two histidine-lysine-aspartate-asparagine-HKDN-(HxKx4Dx6N; x being any amino acid) motifs
evolution
the enzyme belongs to the phospholipase D, PLD, superfamily, which consists of a highly diverse collection of prokaryotic and eukaryotic enzymes, such as bacterial, plant and mammalian PLDs, cardiolipin and phosphatidylserine synthases, Salmonella typhimurium Nuc and mammalian DNase II endonucleases, restriction enzyme BfiI, poxvirus envelope proteins p37K and K4L, and eukaryotic Tdp1, sequence comparison. Family members show the presence of two histidine-lysine-aspartate-asparagine-HKDN-(HxKx4Dx6N; x being any amino acid) motifs
evolution
E2REL5
the enzyme belongs to the phospholipase D, PLD, superfamily, which consists of a highly diverse collection of prokaryotic and eukaryotic enzymes, such as bacterial, plant and mammalian PLDs, cardiolipin and phosphatidylserine synthases, Salmonella typhimurium Nuc and mammalian DNase II endonucleases, restriction enzyme BfiI, poxvirus envelope proteins p37K and K4L, and eukaryotic Tdp1, sequence comparison. Family members show the presence of two histidine-lysine-aspartate-asparagine-HKDN-(HxKx4Dx6N; x being any amino acid) motifs
evolution
the enzyme belongs to the phospholipase D, PLD, superfamily, which consists of a highly diverse collection of prokaryotic and eukaryotic enzymes, such as bacterial, plant and mammalian PLDs, cardiolipin and phosphatidylserine synthases, Salmonella typhimurium Nuc and mammalian DNase II endonucleases, restriction enzyme BfiI, poxvirus envelope proteins p37K and K4L, and eukaryotic Tdp1, sequence comparison. Family members show the presence of two histidine-lysine-aspartate-asparagine-HKDN-(HxKx4Dx6N; x being any amino acid) motifs
evolution
the enzyme belongs to the phospholipase D, PLD, superfamily, which consists of a highly diverse collection of prokaryotic and eukaryotic enzymes, such as bacterial, plant and mammalian PLDs, cardiolipin and phosphatidylserine synthases, Salmonella typhimurium Nuc and mammalian DNase II endonucleases, restriction enzyme BfiI, poxvirus envelope proteins p37K and K4L, and eukaryotic Tdp1, sequence comparison. Family members show the presence of two histidine-lysine-aspartate-asparagine-HKDN-(HxKx4Dx6N; x being any amino acid) motifs
evolution
the enzyme belongs to the phospholipase D, PLD, superfamily, which consists of a highly diverse collection of prokaryotic and eukaryotic enzymes, such as bacterial, plant and mammalian PLDs, cardiolipin and phosphatidylserine synthases, Salmonella typhimurium Nuc and mammalian DNase II endonucleases, restriction enzyme BfiI, poxvirus envelope proteins p37K and K4L, and eukaryotic Tdp1, sequence comparison. Family members show the presence of two histidine-lysine-aspartate-asparagine-HKDN-(HxKx4Dx6N; x being any amino acid) motifs, three-dimensional structural comparison of four PLD superfamily members, overview
evolution
the enzyme belongs to the phospholipase D, PLD, superfamily, which consists of a highly diverse collection of prokaryotic and eukaryotic enzymes, such as bacterial, plant and mammalian PLDs, cardiolipin and phosphatidylserine synthases, Salmonella typhimurium Nuc and mammalian DNase II endonucleases, restriction enzyme BfiI, poxvirus envelope proteins p37K and K4L, and eukaryotic Tdp1, sequence comparison. Family members show the presence of two histidine-lysine-aspartate-asparagine-HKDN-(HxKx4Dx6N; x being any amino acid) motifs, three-dimensional structural comparison of PLD superfamily members, overview
evolution
the enzyme is a member of the metallophosphoesterase enzyme family, the molecular mass of secreted SMPDL3A is tissue and/or species dependent
evolution
the enzyme is a member of the metallophosphoesterase enzyme family, the molecular mass of secreted SMPDL3A is tissue and/or species dependent
evolution
-
the enzyme is a member of the phospholipase D superfamily of enzymes that catalyze the hydrolysis of a variety of phosphodiester bonds in many different substrates
evolution
-
the enzyme is phylogenetically conserved
evolution
-
the enzymes belongs to the ectonucleotide pyrophosphatase/phosphodiesterase (NPP) family
evolution
-
tyrosyl-DNA phosphodiesterase I is a member of the phospholipase D superfamily of enzymes
evolution
-
the enzyme belongs to the phospholipase D, PLD, superfamily, which consists of a highly diverse collection of prokaryotic and eukaryotic enzymes, such as bacterial, plant and mammalian PLDs, cardiolipin and phosphatidylserine synthases, Salmonella typhimurium Nuc and mammalian DNase II endonucleases, restriction enzyme BfiI, poxvirus envelope proteins p37K and K4L, and eukaryotic Tdp1, sequence comparison. Family members show the presence of two histidine-lysine-aspartate-asparagine-HKDN-(HxKx4Dx6N; x being any amino acid) motifs, three-dimensional structural comparison of PLD superfamily members, overview
-
evolution
-
the enzyme is a member of the metallophosphoesterase enzyme family, the molecular mass of secreted SMPDL3A is tissue and/or species dependent
-
malfunction
-
PC-1 is the major source of the elevated phosphate levels in chondrocytes and fibroblasts of patients with familial calcium pyrophosphate dehydrate deposition disease, CPPD. CPPD crystals may be a hallmark of the pathology of osteoarthritis
malfunction
-
Pde1c-/- and Pde4a-/- knockout mutants to examine the role of the PDEs in olfactory transduction. Pde1c-/- OSNs (olfactory sensory neuron cilia) show reduced sensitivity and attenuated adaptation to repeated stimulation, suggesting that PDE1C may be involved in regulating sensitivity and adaptation
malfunction
a loss-of-function AtTDP mutation displays developmental defects and dwarf phenotype in Arabidopsis. This phenotype is substantially caused by decreased cell numbers without any change of individual cell sizes. The tdp plants exhibit hypersensitivities to camptothecin, a potent topoisomerase I inhibitor, and show rigorous cell death in cotyledons and rosette leaves, suggesting the failure of DNA damage repair in tdp mutants
malfunction
-
mutations of the Tdp1 gene are involved in the disease spinocerebellar ataxia with axonal neuropathy
malfunction
-
phosphodiesterase-1 inhibition decreases vascular contraction in arteries from angiotensin II hypertensive, but not control, rats
malfunction
-
aberrant nucleotide pyrophosphatase/phosphodiesterase-1 (NPP1) activity is associated with chondrocalcinosis, osteoarthritis, and type 2 diabetes
malfunction
deletion of the enzyme in budding yeast leads to an increase in Topo1-dependent cytotoxicity either induced by expression of the toxic Topo1T722A mutant enzyme or cells treated with camptothecin
malfunction
Tdp1-/- enzyme knockout mice do not show increased sensitivity to etoposide, i.e. VP16
malfunction
-
Tdp1-knock-out Gallus gallus DT40 cells are hypersensitive to camptothecin and bleomycin but also to etoposide, methyl methanesulfonate, H2O2, and ionizing radiation and they are deficient in mitochondrial enzyme activity, phenotype, overview
malfunction
-
the c03958 insertion gene gkt disruption mutant of TDP1 is generally healthy and fertile, but females exhibit reduced lifespan and diminished climbing ability. Insertion mutant c03958 larvae are exposed to bleomycin, an agent that produces oxidative DNA damage, or topoisomerase I-targeted drugs (camptothecin and a noncamptothecin indenoisoquinoline derivative, LMP-776), survivors display rough eye patches, which are rescued by neuronal expression of wild-type enzyme TDP1, overview
malfunction
the mutation H493R forms the molecular basis for the autosomal recessive neurodegenerative disease spinocerebellar ataxia with axonal neuropathy, SCAN1, and results in an increased stability of its Tdp1-DNA reaction intermediate, overview. Enzyme inhibition might potentiate camptothecin-based chemotherapy, overview
malfunction
-
whilst the enzyme mutants H493R (SCAN1) and H263A retain the ability to bind an apurinic/apyrimidinic site-containing DNA, both mutants do not reveal endonuclease activity
malfunction
enzyme knockdown cells are hypersensitive to etoposide. Late, but not early double-stranded break signaling response is altered in human cells lacking the enzyme. Enzyme knockdown impairs the repair of topoisomerase II-induced DNA double-stranded breaks
malfunction
-
deletion of the enzyme in budding yeast leads to an increase in Topo1-dependent cytotoxicity either induced by expression of the toxic Topo1T722A mutant enzyme or cells treated with camptothecin
-
metabolism
(R,S)-isoproterenol decreases the amount of ecto-nucleotide pyrophosphatase/phosphodiesterase 1 protein by 75% and 81%, respectively. Contrary to downregulation of ecto-nucleotide pyrophosphatase/phosphodiesterase 1, an upregulation of glial fibrillary acidic protein, a differentiation marker for astrocytic cells is observed. Ca2+, PKA, PI 3-K/PKB/GSK-3, Epac/Rap1/PP2A and MAP kinase modules are not involved in the inhibition of ecto-nucleotide pyrophosphatase/phosphodiesterase 1 gene expression, overview
metabolism
-
TDP1 knockdown does not produce a change in sensitivity to camptothecin, whereas co-silencing of other pathways cooperating with TDP1 in cell response to topoisomerase I poisons indicates that XRCC1 and BRCA1 are major regulators of sensitivity
metabolism
-
the tyrosyl-DNA phosphodiesterase I hydrolyzes the phosphotyrosyl linkage between degraded Top1 and DNA, then polynucleotide kinase phosphatase hydrolyzes the resulting 3'-phosphate end and catalyzes the phosphorylation of the 5'-hydroxyl end of the broken DNA strand. This results in a broken DNA strand with termini consisting of a 5'-phosphate and 3'-hydroxyl for DNA repair. DNA polymerase beta replaces the missing DNA segment, and finally DNA ligase III reseals the broken DNA. Tyrosyl-DNA phosphodiesterase I is the only enzyme that specifically catalyzes the hydrolysis of the phosphodiester bond between the catalytic Tyr723 of Top1 and DNA-3'-phosphate
metabolism
-
(R,S)-isoproterenol decreases the amount of ecto-nucleotide pyrophosphatase/phosphodiesterase 1 protein by 75% and 81%, respectively. Contrary to downregulation of ecto-nucleotide pyrophosphatase/phosphodiesterase 1, an upregulation of glial fibrillary acidic protein, a differentiation marker for astrocytic cells is observed. Ca2+, PKA, PI 3-K/PKB/GSK-3, Epac/Rap1/PP2A and MAP kinase modules are not involved in the inhibition of ecto-nucleotide pyrophosphatase/phosphodiesterase 1 gene expression, overview
-
physiological function
-
PC-1 is an enzymatic generator of diphosphate and a critical regulator of tissue mineralization
physiological function
AtTDP plays a clear role in the repair of topoisomerase I-DNA complexes in Arabidopsis, the tyrosyl-DNA phosphodiesterase 1 is a key enzyme that hydrolyzes the phosphodiester bond between tyrosine of topoisomerase and 3'-phosphate of DNA and repairs topoisomerase-mediated DNA damage during chromosome metabolism. Recombinant AtTDP protein certainly hydrolyzes the 3'-phosphotyrosyl DNA substrates related to repairing in vivo topoisomerase I-DNA-induced damage
physiological function
-
phosphodiesterase 1 plays a role in decreased cGMP level contributing to increased contraction in arteries from hypertensive rats. Ang II augments PDE1 activation, decreasing the bioavailability of cyclic guanosine 3',5'-monophosphate, and contributing to increased vascular contractility, effects of different PDF isozymes, overview
physiological function
-
role and underlying mechanism of cyclic nucleotide phosphodiesterase 1, PDE1, in regulating collagen I in synthetic vascular smooth muscle cells, overview
physiological function
-
role of Tdp1 in the new APE-independent base excision repair pathway in mammals
physiological function
th enzyme participates in topoisomerase I-mediated DNA damage repair process and thereby counteracts the cytotoxic effect of topoisomerase I inhibitors
physiological function
-
tyrosyl-DNA phosphodiesterase 1 catalyses the hydrolysis of phosphodiester linkages between a DNA 3' phosphate and a tyrosine residue as well as a variety of other DNA 3 substituents, and is implicated in the repair of covalent complexes involving eukaryotic type IB topoisomerases. Processing by the proteasome is required for TDP1 cleavage in vivo
physiological function
-
tyrosyl-DNA phosphodiesterase 1 is a key enzyme that hydrolyzes the phosphodiester bond between tyrosine of topoisomerase and 3'-phosphate of DNA and repairs topoisomerase-mediated DNA damage during chromosome metabolism
physiological function
-
tyrosyl-DNA phosphodiesterase 1 is an enzyme vital to the repair of covalent DNA-topoisomerase adducts, e.g. induced by the mycotoxin alternariol, it affects alternariol-mediated genotoxicity. TDP1 plays an important role in the repair of topoisomerase-mediated DNA damage. The repair enzyme TDP1 is a factor for the modulation of AOH-mediated DNA damage in human cells. TDP1 is also involved in the repair of topoisomerase II-induced DNA damage
physiological function
-
tyrosyl-DNA phosphodiesterase 1 plays a unique function as it catalyzes the repair of topoisomerase I-mediated DNA damage. TDP1 alone can account for mild levels of camptothecin resistance, repair of topoisomerase I-mediated DNA damage likely occurs through redundant pathways mainly implicating BRCA1 and XRCC1, but not RAD17 and PARP1
physiological function
-
human tyrosyl-DNA phosphodiesterase 1 catalyzes the apurinic/apyrimidinic site cleavage reaction to generate breaks with the 3'- and 5'-phosphate termini. The enzyme activity can contribute to the repair of apurinic/apyrimidinic sites particularly in DNA structures containing ssDNA region or apurinic/apyrimidinic sites in the context of clustered DNA lesions
physiological function
SMPDL3A is the major nucleotide phosphodiesterase secreted by human THP-1 macrophages after LXR stimulation, it may play a novel role in the pathobiology of atherosclerosis. SMPDL3A is a major source of nucleotide phosphodiesterase activity secreted by LXR-stimulated human macrophages, enzyme expression and secretion is regulated by intracellular cAMP, and is regulated by liver X receptor, LXR,. The CREs in the promoter region of SMPDL3A may play a functional role in primary human macrophages. The enzyme is capable of hydrolyzing sphingomyelin in oxidized LDL particles, transforming them into a more aggregation prone form which is more readily retained by arterial proteoglycans. But SMPDL3A is not an acid sphingomyelinase, but unexpectedly is active against nucleotide diphosphate and triphosphate substrates at acidic and neutral pH
physiological function
-
the enzyme is critical for neuroprotection, normal longevity, and repair of damaged DNA through the removal of blocking lesions at the 3'-ends of DNA or RNA
physiological function
-
the enzyme plays a critical role in the cellular repair of topoisomerase 1-mediated DNA damage
physiological function
-
the enzyme plays a key role in the repair of damaged DNA resulting from the topoisomerase I inhibitor camptothecin and a variety of other DNA-damaging anticancer agents
physiological function
-
tyrosyl-DNA phosphodiesterase 1 repairs topoisomerase I cleavage complexes by hydrolyzing their 3'-phosphotyrosyl DNA bonds and repairs bleomycin-induced DNA damage by hydrolyzing 3'-phosphoglycolates
physiological function
-
tyrosyl-DNA phosphodiesterase 1 repairs topoisomerase I cleavage complexes by hydrolyzing their 3'-phosphotyrosyl DNA bonds and repairs bleomycin-induced DNA damage by hydrolyzing 3'-phosphoglycolates. The yeast enzyme is also implicated in the repair of topoisomerase II-DNA cleavage complexes. The enzyme and CtIP act in parallel pathways for the repair of topoisomerase I cleavage complexes and methyl methanesulfonate-induced lesions but are epistatic for topoisomerase II cleavage complexes
physiological function
tyrosyl-DNA phosphodiesterase I is a eukaryotic DNA repair enzyme that catalyzes the removal of covalent 3'-DNA adducts, the enzyme hydrolyzes the 3'-phospho-tyrosyl that in the cell covalently links DNA topoisomerase I and DNA
physiological function
E2REL5
tyrosyl-DNA phosphodiesterase I is a eukaryotic DNA repair enzyme that catalyzes the removal of covalent 3'-DNA adducts, the enzyme hydrolyzes the 3'-phospho-tyrosyl that in the cell covalently links DNA topoisomerase I and DNA
physiological function
tyrosyl-DNA phosphodiesterase I is a eukaryotic DNA repair enzyme that catalyzes the removal of covalent 3'-DNA adducts, the enzyme hydrolyzes the 3'-phospho-tyrosyl that in the cell covalently links DNA topoisomerase I and DNA
physiological function
tyrosyl-DNA phosphodiesterase I is a eukaryotic DNA repair enzyme that catalyzes the removal of covalent 3'-DNA adducts, the enzyme hydrolyzes the 3'-phospho-tyrosyl that in the cell covalently links DNA topoisomerase I and DNA
physiological function
tyrosyl-DNA phosphodiesterase I is a eukaryotic DNA repair enzyme that catalyzes the removal of covalent 3'-DNA adducts, the enzyme hydrolyzes the 3'-phospho-tyrosyl that in the cell covalently links DNA topoisomerase I and DNA. Phosphorylation of Ser81 regulates hTdp1 targeting to sites of DNA damage and stabilizes its interaction with X-ray repair cross-complementing protein 1 (XRCC1) and/or DNA ligase III similar to how ATM-mediated phosphorylation of PNKP promotes its activity at DNA lesions. The human enzyme expressed in DT40 chicken B-lymphoblast cells plays a protective role against etoposide
physiological function
tyrosyl-DNA phosphodiesterase I is a eukaryotic DNA repair enzyme that catalyzes the removal of covalent 3'-DNA adducts, the enzyme hydrolyzes the 3'-phospho-tyrosyl that in the cell covalently links DNA topoisomerase I and DNA. The enzyme may play a role in chemo-resistance to pharmacologic inhibitors of topoisomerase I
physiological function
tyrosyl-DNA phosphodiesterase I is a eukaryotic DNA repair enzyme that catalyzes the removal of covalent 3'-DNA adducts, the enzyme hydrolyzes the 3'-phospho-tyrosyl that in the cell covalently links DNA topoisomerase I and DNA. The enzyme plays a role in suppressing etoposide-induced DNA damage
physiological function
the enzyme catalyzes the repair of 3'-DNA adducts, such as the 3'-phosphotyrosyl linkage of DNA topoisomerase I to DNA
physiological function
the enzyme plays a key role in the removal of DNA damage resulting from Topo1 inhibition or caused by other anticancer drugs, e.g., temozolomide, bleomycin, etoposide, etc.
physiological function
tyrosyl-DNA-phosphodiesterase 1 is a DNA repair enzyme that removes irreversible protein-linked 3'-DNA complexes, 3'-phosphoglycolates, alkylation damage-induced DNA breaks, and 3'-deoxyribose nucleosides. The enzyme plays an active role in the repair of topoisomerase II-induced DNA damage
physiological function
-
phosphodiesterase 1 plays a role in decreased cGMP level contributing to increased contraction in arteries from hypertensive rats. Ang II augments PDE1 activation, decreasing the bioavailability of cyclic guanosine 3',5'-monophosphate, and contributing to increased vascular contractility, effects of different PDF isozymes, overview
-
physiological function
-
tyrosyl-DNA phosphodiesterase I is a eukaryotic DNA repair enzyme that catalyzes the removal of covalent 3'-DNA adducts, the enzyme hydrolyzes the 3'-phospho-tyrosyl that in the cell covalently links DNA topoisomerase I and DNA. The enzyme may play a role in chemo-resistance to pharmacologic inhibitors of topoisomerase I
-
additional information
-
knockdown of the enzyme TDP1 in U2-OS cells does not increase sensitivity to gimatecan
additional information
overexpression of the active enzyme protects the parasites against topoisomerase IB inhibitor camptothecin and oxidative agent H2O2-mediated cytotoxicity and its downregulation rendered the parasites hypersensitive to camptothecin. Downregulation of LdTdp1 mRNA occurs because of blockage of transcription rather than increased turnover, transcriptional regulation, overview
additional information
-
overexpression of the active enzyme protects the parasites against topoisomerase IB inhibitor camptothecin and oxidative agent H2O2-mediated cytotoxicity and its downregulation rendered the parasites hypersensitive to camptothecin. Downregulation of LdTdp1 mRNA occurs because of blockage of transcription rather than increased turnover, transcriptional regulation, overview
additional information
-
Tdp1 is known to interact stably with BER proteins: DNA polymerase beta, XRCC1, PARP1 and DNA ligase III
additional information
expression and sequence comparisons, overview
additional information
-
expression and sequence comparisons, overview
additional information
expression and sequence comparisons, overview
additional information
-
the enzyme is composed of two domains related by a pseudo-twofold axis of symmetry. Each domain contributes a histidine and a lysine residue to form an active site that is centrally located at the symmetry axis. Four additional residues N283, Q294, N516, and E538 are also positioned near the active site
additional information
-
expression and sequence comparisons, overview
-
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