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(2'S)-1D-1,2-O-[(2'-phosphoryloxy)propane-1',3'-diyl]-myo-inositol 4,5-bisphosphate
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synthetic bicyclic inositol trisphosphate S epimer, IC50 is 0.156 mM
1D-myo-inositol 1,3,4,5-tetrakisphosphate
1D-myo-inositol 1,4,5-trisphosphate
2,3-diphosphoglycerate
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2-[3,5-dimethyl-1-(4-nitrophenyl)-1H-pyrazol-4-yl]-5,8-dinitro-1H-benzo[de]isoquinoline-1,3(2H)-dione
BIP-4, BIP-4 is competitive to Ins(1,4,5)P3 and shows high selectivity for the Ins(1,4,5)P3 binding pocket, BIP-4 does not block the actin bundling activity of ITPKA
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3',4',7,8-tetrahydroxyflavone
7-methylsulfanyl-3-phenyl-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one
55% inhibition at 0.04 mM
D-2-deoxyinositol 1,3,4,5-tetrakisphosphate
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strong inhibition of isozyme A, IC50 is 0.0054 mM
D-2-deoxyinositol 1,4,5-trisphosphate
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strong inhibition of isozyme A, IC50 is 0.0017 mM
D-3-deoxyinositol 1,4,6-trisphosphate
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strong inhibition of isozyme A, IC50 is 0.0014 mM
D-6-deoxyinositol 1,3,4,5-tetrakisphosphate
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strong inhibition of isozyme A, IC50 is 0.0051 mM
D-myo-inositol 1,4,5-trisphosphate
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strong inhibition, purified recombinant enzyme, IC50 value is 0.003 mM in absence of Ca2+
D-myo-inositol 2,4,5-trisphosphate
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IC50 is 0.117 mM
D-scyllo-inositol 1,2,3,4-tetrakisphosphate
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purified recombinant enzyme, IC50 value is above 0.1 mM in absence of Ca2+
D-scyllo-inositol 1,2,4-trisphosphate
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purified recombinant enzyme, IC50 value is 0.044 mM in absence of Ca2+
epigallocatechin-3-gallate
heparin
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mixed-type inhibition
inositol phosphate
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inhibitory effects of all possible 38 regioisomers of synthetic inositol phosphates, only inositol trisphosphates and tetrakisphosphates inhibit, not or very weak: inositol monophosphates, bisphosphates and pentakisphosphates, the recognition of myo-inositol phosphate regioisomers is highly structure-selective
L-scyllo-inositol 1,2,3,4-tetrakisphosphate
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purified recombinant enzyme, IC50 value is above 0.1 mM in absence of Ca2+
L-scyllo-inositol 1,2,4-trisphosphate
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purified recombinant enzyme, IC50 value is 0.006 mM in absence of Ca2+
N-(1,2-benzoxazol-3-yl)-4-methylbenzamide
68% inhibition at 0.04 mM, mixed type inhibitor, that is nearly completely taken up by H1299 cells and remains stable after cellular uptake, the compound exhibits a robust stability and a high membrane permeability. The inhibitor provides the possibility to partly inhibit the metastasis-promoting effect of ITPKA in lung tumor cells. Inhibition mechanism of BAMB-4, overview
N-(4-ethoxyphenyl)pyrazolo[1,5-a]pyridine-3-carboxamide
87% inhibition at 0.04 mM
N-(6-Aminohexyl)-5-chloro-1-naphthalenesulfonamide
protein kinase A
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isoforms A and B are differentially regulated via phosphorylation by the cAMP-dependent protein kinase, isoform A: stimulation in the presence or absence of Ca2+/calmodulin, isoform B: no effect on activity in the absence of Ca2+/calmodulin, 45% inhibition in the presence of Ca2+/calmodulin
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RS-20
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calmodulin antagonist, prevents the Ca2+/calmodulin-mediated activation
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scyllo-inositol 1,2,3,5-tetrakisphosphate
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weak inhibition, purified recombinant enzyme, IC50 value is 0.028 mM in absence of Ca2+
scyllo-inositol 1,2,3-trisphosphate
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purified recombinant enzyme, IC50 value is 0.027 mM in absence of Ca2+
scyllo-inositol 1,2,4,5-tetrakisphosphate
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weak inhibition, purified recombinant enzyme, IC50 value is 0.039 mM in absence of Ca2+
scyllo-inositol 1,3,5-trisphosphate
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purified recombinant enzyme, IC50 value is 0.090 mM in absence of Ca2+
TSH
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thyroid-stimulating hormone, inhibits at a physiological concentration, inhibition is mimicked by dibuturyl cyclic AMP and forskolin, mechanism
1D-myo-inositol 1,3,4,5-tetrakisphosphate
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marked product inhibition, isoforms A and B
1D-myo-inositol 1,3,4,5-tetrakisphosphate
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product inhibition, IC50 is 0.013 mM
1D-myo-inositol 1,4,5-trisphosphate
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substrate inhibition of the catalytic domain
1D-myo-inositol 1,4,5-trisphosphate
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recombinant, catalytically active fragment of isoform C, substrate inhibition by high concentrations
3',4',7,8-tetrahydroxyflavone
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mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate
3',4',7,8-tetrahydroxyflavone
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the point mutant K336Q reveals a drastically reduced inhibition by THF. Substitution of Lys336 leads to a 260fold increase in the IC50. On the other hand, kinetic parameters of the enzyme with respect to both substrates are nearly unchanged. This region shows high homology between IP3K isoforms.
3',4',7,8-tetrahydroxyflavone
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inhibition of isozyme A, mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate
3',4',7,8-tetrahydroxyflavone
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3',4',7,8-tetrahydroxyflavone
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mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate
3',4',7,8-tetrahydroxyflavone
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aurintricarboxylic acid
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mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate
aurintricarboxylic acid
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aurintricarboxylic acid
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inhibition of isozyme A and isozyme B, mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate
aurintricarboxylic acid
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aurintricarboxylic acid
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strong inhibition, mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate
aurintricarboxylic acid
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Ca2+
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Ca2+
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at concentrations higher than 0.01-0.1 mM
Ca2+
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at higher concentrations
Ca2+
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isoforms A and B, above 0.01 mM
chlorogenic acid
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chlorpromazine
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calmodulin-antagonist, inhibits Ca2+-activated enzyme activity
chlorpromazine
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calmodulin-antagonist, inhibits Ca2+-activated enzyme activity
EGTA
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Ca2+/calmodulin-activated enzyme
EGTA
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Ca2+/calmodulin-activated enzyme
EGTA
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Ca2+/calmodulin-activated enzyme
EGTA
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Ca2+/calmodulin-activated enzyme
ellagic acid
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mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate
ellagic acid
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inhibition of isozyme B, slight inhibition of isozyme A, mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate
epicatechin-3-gallate
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mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate
epicatechin-3-gallate
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epicatechin-3-gallate
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slight inhibition of isozyme A and isozyme B, mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate
epicatechin-3-gallate
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mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-triphosphate
epigallocatechin-3-gallate
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mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate
epigallocatechin-3-gallate
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epigallocatechin-3-gallate
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inhibition of isozyme A, mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate
epigallocatechin-3-gallate
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epigallocatechin-3-gallate
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mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-triphosphate
epigallocatechin-3-gallate
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gossypol
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mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate
gossypol
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inhibition of isozyme A and isozyme B, mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate
gossypol
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mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate
hypericin
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mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate
hypericin
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inhibition of isozyme A and isozyme B, mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate
hypericin
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mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-triphosphate
KN-62
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calmodulin-dependent protein kinase II inhibitor; prevents the carbachol- or UTP-mediated activation
KN-62
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calmodulin-dependent protein kinase II inhibitor; prevents the carbachol- or UTP-mediated activation
KN-62
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calmodulin-dependent protein kinase II inhibitor; prevents the Ca2+/calmodulin-mediated activation
KN-93
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calmodulin-dependent protein kinase II inhibitor; prevents the carbachol- or UTP-mediated activation
KN-93
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calmodulin-dependent protein kinase II inhibitor; prevents the carbachol- or UTP-mediated activation
KN-93
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calmodulin-dependent protein kinase II inhibitor; prevents the Ca2+/calmodulin-mediated activation
myricetin
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mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate
myricetin
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inhibition of isozyme A, mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate
myricetin
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mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate
N-(6-Aminohexyl)-5-chloro-1-naphthalenesulfonamide
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i.e. W-7, calmodulin-antagonist; inhibits Ca2+-activated enzyme activity
N-(6-Aminohexyl)-5-chloro-1-naphthalenesulfonamide
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i.e. W-7, calmodulin-antagonist
N-(6-Aminohexyl)-5-chloro-1-naphthalenesulfonamide
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i.e. W-7, calmodulin-antagonist; inhibits Ca2+-activated enzyme activity
Protein kinase C
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phosphorylates and inactivates enzyme
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Protein kinase C
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phosphorylates and inactivates enzyme
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Protein kinase C
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negative regulatory function, phosphorylates the enzyme at a serine residue
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Protein kinase C
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protein kinase C alone, without CaM kinase II, inhibits in the presence of Ca2+ and calmodulin
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Protein kinase C
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isoforms A and B are differentially regulated via phosphorylation by protein kinase C, isoform A: phosphorylated to the extent of 2 mol/mol, 72% inhibition in the absence of Ca2+/calmodulin, isoform B: phosphorylated to the extent of 2.7 mol/mol, no effect on activity in the absence of Ca2+/calmodulin, both isoforms are inhibited by 70% in the presence of Ca2+/calmodulin
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Protein kinase C
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negative regulatory function, phosphorylates the enzyme at Ser175, simultaneous phosphorylation at Ser109 and Ser175 also inactivates the enzyme
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Protein kinase C
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negative regulatory function, phosphorylates the enzyme at a Ser residue
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quercetin
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mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate
quercetin
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inhibition of isozyme A, mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate
quercetin
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mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate
Rose bengal
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Rose bengal
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slight inhibition of isozyme B, mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate
SDS
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complete inhibition at 0.1%, 1% Triton X-100 partially reverses
additional information
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IC50 values, overiew, the inhibition by the synthetic or plant phenols can in some cases be partially or completely reversed by Triton X-100, no inhibition by chlorogenic acid and by Rose Bengal
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additional information
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All inhibitors display a mixed-type inhibition with respect to ATP and a noncompetitive inhibition with respect to 1D-myo-inositol 1,4,5-triphosphate. Mutagenesis studies reveal that both the calmodulin binding and the ATP binding domains in IP3K are involved in inhibitor binding. Most discovered potent IP3K inhibitors exert antiproliferative effects on cultured cells in vitro or in animal experiments and tumor treatment studies in vivo.; Reversal of enzyme inhibition by addition of Triton X-100 and Ca2+-calmodulin.
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additional information
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IC50 values, overiew, inhibitory potency of the synthetic and plant phenolics, no inhibition by chlorogenic acid
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additional information
All inhibitors display a mixed-type inhibition with respect to ATP and a noncompetitive inhibition with respect to inositol-1,4,5-trisphosphate. Mutagenesis studies reveal that both the calmodulin binding and the ATP binding domains in IP3K are involved in inhibitor binding. Most discovered potent IP3K inhibitors exert antiproliferative effects on cultured cells in vitro or in animal experiments and tumor treatment studies in vivo.; All inhibitors display a mixed-type inhibition with respect to ATP and a noncompetitive inhibition with respect to Ins(1,4,5)P3. Mutagenesis studies reveal that both the calmodulin binding and the ATP binding domains in IP3K are involved in inhibitor binding. Most discovered potent IP3K inhibitors exert antiproliferative effects on cultured cells in vitro or in animal experiments and tumor treatment studies in vivo.
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additional information
All inhibitors display a mixed-type inhibition with respect to ATP and a noncompetitive inhibition with respect to inositol-1,4,5-trisphosphate. Mutagenesis studies reveal that both the calmodulin binding and the ATP binding domains in IP3K are involved in inhibitor binding. Most discovered potent IP3K inhibitors exert antiproliferative effects on cultured cells in vitro or in animal experiments and tumor treatment studies in vivo.; All inhibitors display a mixed-type inhibition with respect to ATP and a noncompetitive inhibition with respect to Ins(1,4,5)P3. Mutagenesis studies reveal that both the calmodulin binding and the ATP binding domains in IP3K are involved in inhibitor binding. Most discovered potent IP3K inhibitors exert antiproliferative effects on cultured cells in vitro or in animal experiments and tumor treatment studies in vivo.
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additional information
in order to inhibit the metastasis-promoting activity of ITPKA, both its actin bundling and its InsP3kinase activity has to be blocked, inhibitor library screening, overview
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additional information
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not inhibited by GTP or 5'-guanylylimidodiphosphate
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additional information
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enzyme contains several motifs susceptible to a variety of proteases
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additional information
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inhibitor binding structures and mechanism, scyllo-inositol pentakisphosphate, scyllo-inositol hexakisphosphate, scyllo-inositol monophosphate, and scyllo-inositol S-bisphosphates are poor inhibitors
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additional information
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poor inhibition by adenophostin analogues xylo-furanophostin and furanophostin, by L-myo-inositol 2,4,5-trisphosphate, synthetic bicyclic inositol trisphosphate R epimer, and by epi-1D-myo-inositol 1,3,6-trisphosphate
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additional information
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IC50 values, overiew, no inhibition by chlorogenic acid, poor inhibition by rose bengal, and ellagic acid
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additional information
All inhibitors display a mixed-type inhibition with respect to ATP and a noncompetitive inhibition with respect to 1D-myo-inositol 1,4,5-triphosphate. Mutagenesis studies reveal that both the calmodulin binding and the ATP binding domains in IP3K are involved in inhibitor binding. Most discovered potent IP3K inhibitors exert antiproliferative effects on cultured cells in vitro or in animal experiments and tumor treatment studies in vivo.; The flavonoids myricetin, 3',4',7,8-tetrahydroxyflavone, and epigallocatechin-3-gallate have a markedly stronger effect on isoforms A and C than on isoform B
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