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2.1.1.63: methylated-DNA-[protein]-cysteine S-methyltransferase

This is an abbreviated version!
For detailed information about methylated-DNA-[protein]-cysteine S-methyltransferase, go to the full flat file.

Word Map on EC 2.1.1.63

Reaction

DNA (containing 4-O-methylthymine)
+
protein L-cysteine
=
DNA (without 4-O-methylthymine)
+
protein S-methyl-L-cysteine

Synonyms

Ada protein, Ada-C, AGAT, AGT, AGTendoV, alkylated DNA-protein alkyltransferase, alkylguanine transferase, ATASE, C-hAGT, carboxyl terminal domain of the inducible Escherichia coli ada alkyltransferase, hAGT, methylated-DNA-[protein]-cysteine S-methyltransferase, methylguanine DNA methyltransferase, MGMT, Mgt1, MJ1529, N-hAGT, O6-alkylguanine DNA alkyltransferase, O6-alkylguanine DNA-alkyltransferase, O6-alkylguanine-DNA alkyl-transferase, O6-alkylguanine-DNA alkyltransferase, O6-methylguanine DNA methyltransferase, O6-methylguanine methyltransferase, O6-methylguanine-DNA methyltransferase, O6-methylguanine-DNA-methyltransferase, O6-MGMT, O6meG-DNA alkyltransferase, OGT, Pk-MGMT, SSO2487, Tk-MGMT, TTHA1564

ECTree

     2 Transferases
         2.1 Transferring one-carbon groups
             2.1.1 Methyltransferases
                2.1.1.63 methylated-DNA-[protein]-cysteine S-methyltransferase

Inhibitors

Inhibitors on EC 2.1.1.63 - methylated-DNA-[protein]-cysteine S-methyltransferase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
2-([2-amino-6-[(4-bromothiophen-2-yl)methoxy]-9H-purin-9-yl]methoxy)ethanol
-
-
2-amino-O4-benzyl-6,7-dimethylpteridine
-
potent
2-amino-O4-benzyl-6-formylpteridine
-
potent
2-amino-O4-benzyl-6-hydroxymethylpteridine
-
potent
2-amino-O4-benzylpteridine
-
potent
2-amino-O4-benzylpteridine-6-carboxylic acid
-
potent
2-hexaprenyl-6-methoxy-1,4-benzoquinone
-
-
4-[(4-bromothiophen-2-yl)methoxy]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
-
-
4-[bis(2-chloroethyl)amino]-L-phenylalanine
-
hyperthermia enhances the inhibitory effects of L-phenylalanine mustard on melanoma cell growth
6-(1-benzofuran-2-ylmethoxy)-9H-purin-2-amine
-
-
6-(4,5,6,7-tetrahydro-1-benzothiophen-2-ylmethoxy)-9H-purin-2-amine
-
-
6-(naphtho[1,2-b]thiophen-2-ylmethoxy)-9H-purin-2-amine
-
-
6-(naphtho[2,1-b]thiophen-2-ylmethoxy)-9H-purin-2-amine
-
-
6-(phenanthro[9,10-b]thiophen-2-ylmethoxy)-9H-purin-2-amine
-
-
6-O-benzylguanine
6-[(1-methyl-4-nitro-1H-pyrrol-2-yl)methoxy]-9H-purin-2-amine
-
-
6-[(4-bromothiophen-2-yl)methoxy]-9-(2-deoxy-beta-D-erythro-pentofuranosyl)-9H-purin-2-amine
-
-
7-[(4-bromothiophen-2-yl)methoxy]-2,3-dihydro-1H-[1,2,3]triazolo[4,5-d]pyrimidin-5-amine
-
-
9-beta-D-arabinofuranosyl-6-[(4-bromothiophen-2-yl)methoxy]-9H-purin-2-amine
-
-
alkyltransferase-like protein
inhibits the transfer of methyl groups to MGMT, thus the action of MGMT on 6-O-methylguanine in DNA, inhibition is reversible by prolonged incubation in the presence of MGMT
-
Br(CH2)2Br
-
inactivates purified AGT and mutant R128A to approximately the same extent; inactivates purified AGT and mutant R128A to approximately the same extent, small reduction in the loss of activity in the absence of DNA, but no effect at all in the presence of DNA, inactivates mutant Y114A much less than wild-type, and DNA completely prevents this inactivation, mutants P140K and Y158H are less inactivated than wild-type AGT, specifically in the presence of DNA
Br(CH2)3Br
-
mutant P140K requires higher concentrations than wild-type AGT for inactivation
Br(CH2)5Br
-
mutant P140K requires higher concentrations than wild-type AGT for inactivation
BrCH2Br
-
wild-type AGT and mutant P140K show no difference in sensitivity to BrCH2Br
BrCH2OAc
-
reacts with the enzyme at its cysteine acceptor site, abolishing its DNA repair activity, the formation of AGT-Cys145S-CH2Br by BrCH2OAc
CH2Br2
-
reacts with the enzyme at its cysteine acceptor site, abolishing its DNA repair activity
DNA (containing 6-O-carboxymethylguanine)
-
-
-
DNA (containing 6-O-methylguanine)
-
-
double-stranded oligonucleotides
-
6-O-methylguanine, 6-O-(4-fluorobenzyl)-guanine, 6-O-(3-fluorobenzyl)-guanine, 6-O-(2-fluorobenzyl)-guanine, 6-O-benzylguanine, 6-O-benzylhypoxanthine. IC50: 1.4-3.0 nM
-
formaldehyde
-
decreases activity at levels up to 3fold higher than the maximally allowed workplace concentration, no decrease at the maximally allowed level
methotrexate
-
-
methyl bromide
methyl iodide
-
can directly alkylate the active site of the enzyme, the agent can increase the effectiveness of environmental and endogenously produced alkylating carcinogens in producing the mutagenic 6-O-alkylguanine residue in DNA in vivo
methyl isocyanate
-
methyl isocyanate resulting from base-catalyzed activation of VNP40101M inhibits the enzyme, thereby enhancing the yield of the DNA G-C interstrand crosslink responsible for the antitumor activity of this agent
N9-cyclopentyl-O6-(4-bromothenyl)guanine
efficient inhibitor of wild-type AGT
Na2SO4
Na3 citrate
Ni2+
-
purified protein is not very sensitive to this metal but the loss of AGT could contribute to the well-known carcinogenicity of nickel
O(6)-benzylguanine
-
BG
O4-(4-bromothenylpterin)
-
-
O4-benzylfolic acid
-
30times more active than O6-benzylguanine against the wild-type alkyltransferase, inactivation of P140K mutant alkyltransferase. Inhibitor shows promise as an agent for possible tumor-selective alkyltransferase inactivation superior toO6-benzylguanine as a chemotherapy adjuvant
O6-(1,2-thiazol-4-ylmethyl)guanine
-
-
O6-(1,3-oxazol-5-yl)guanine
-
-
O6-(1,3-thiazol-5-yl)guanine
-
-
O6-(1-benzofuran-2-ylmethyl)guanine
-
-
O6-(2-benzo[b]thienylmethyl)guanine
-
-
O6-(3-pyridyl)guanine
-
-
O6-(4-(2-chloropyridyl))guanine
-
-
O6-(4-bromothenyl)-8-oxaguanine
-
-
O6-(4-bromothenyl)-8-thiaguanine
-
-
O6-(4-bromothenyl)guanine
O6-(4-pyridyl)guanine
-
-
O6-alkylating drugs
-
O6-alkylating drugs deplete MGMT activity indirectly via alkylation of DNA
-
O6-benzyl guanine
-
-
O6-benzyl-2'-deoxyguanosine
-
-
O6-benzylguanine
O6-furfurylguanine
-
-
O6-methylguanine
-
-
O6-methylguanine oligonucleotide
-
O6-thenylguanine
-
original Patrin, became Patrin-1
O6-[(1-methyl-1H-imidazol-5-yl)methyl]guanine
-
-
temozolomide
VNP40101M
-
methyl isocyanate resulting from base-catalyzed activation of VNP40101M inhibits the enzyme, thereby enhancing the yield of the DNA G-C interstrand crosslink responsible for the antitumor activity of this agent
additional information
-