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Literature summary for 2.7.1.127 extracted from
- Antiproliferative plant and synthetic polyphenolics are specific inhibitors of vertebrate inositol-1,4,5-trisphosphate 3-kinases and inositol polyphosphate multikinase (2005), J. Biol. Chem., 280, 13229-13240.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| cloning of isozyme IP3K-A from erythrocytes and expression of a fragment comprising the catalytic domain and the CaM binding domain of the wild-type and mutant enzyme, respectively, in Escherichia coli strain BL21(DE3) | Gallus gallus |
| isozymes IP3K-A and IP3K-B, expression of a fragment comprising the catalytic domain and the CaM binding domain, residues 165-462 of isozyme A, of the wild-type and mutant isozyme A and isozyme B, respectively, in Escherichia coli strain BL21(DE3) | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| K268E | site-directed mutagenesis, activity is similar to the wild-type enzyme, the sensitivity to inhibitor 3',4',7,8-tetrahydroxyflavone is highly reduced compared to the wild-type enzyme | Gallus gallus |
| K272D | site-directed mutagenesis, activity is similar to the wild-type enzyme, the sensitivity to inhibitor 3',4',7,8-tetrahydroxyflavone is highly reduced compared to the wild-type enzyme | Gallus gallus |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 3',4',7,8-tetrahydroxyflavone | mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate | Gallus gallus |  |
| 3',4',7,8-tetrahydroxyflavone | inhibition of isozyme A, mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate | Homo sapiens | |
| 3',4',7,8-tetrahydroxyflavone | mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate | Rattus norvegicus | |
| aurintricarboxylic acid | mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate | Gallus gallus | |
| aurintricarboxylic acid | inhibition of isozyme A and isozyme B, mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate | Homo sapiens | |
| aurintricarboxylic acid | strong inhibition, mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate | Rattus norvegicus | |
| ellagic acid | mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate | Gallus gallus | |
| ellagic acid | inhibition of isozyme B, slight inhibition of isozyme A, mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate | Homo sapiens | |
| epicatechin-3-gallate | mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate | Gallus gallus | |
| epicatechin-3-gallate | slight inhibition of isozyme A and isozyme B, mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate | Homo sapiens | |
| epicatechin-3-gallate | mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-triphosphate | Rattus norvegicus | |
| epigallocatechin-3-gallate | mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate | Gallus gallus | |
| epigallocatechin-3-gallate | inhibition of isozyme A, mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate | Homo sapiens | |
| epigallocatechin-3-gallate | mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-triphosphate | Rattus norvegicus | |
| gossypol | mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate | Gallus gallus | |
| gossypol | inhibition of isozyme A and isozyme B, mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate | Homo sapiens | |
| gossypol | mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate | Rattus norvegicus | |
| hypericin | mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate | Gallus gallus | |
| hypericin | inhibition of isozyme A and isozyme B, mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate | Homo sapiens | |
| hypericin | mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-triphosphate | Rattus norvegicus | |
| additional information | 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 | Gallus gallus | |
| additional information | IC50 values, overiew, inhibitory potency of the synthetic and plant phenolics, no inhibition by chlorogenic acid | Homo sapiens | |
| additional information | IC50 values, overiew, no inhibition by chlorogenic acid, poor inhibition by rose bengal, and ellagic acid | Rattus norvegicus | |
| myricetin | mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate | Gallus gallus | |
| myricetin | inhibition of isozyme A, mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate | Homo sapiens | |
| myricetin | mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate | Rattus norvegicus | |
| quercetin | mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate | Gallus gallus | |
| quercetin | inhibition of isozyme A, mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate | Homo sapiens | |
| quercetin | mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate | Rattus norvegicus | |
| Rose bengal | slight inhibition of isozyme B, mixed-type versus ATP, noncompetitive versus 1D-myo-inositol 1,4,5-trisphosphate | Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0002 | - |
1D-myo-inositol 1,4,5-trisphosphate | recombinant catalytic/CaM binding domain, pH 7.5, 30°C | Rattus norvegicus | |
| 0.0004 | - |
1D-myo-inositol 1,4,5-trisphosphate | recombinant wild-type catalytic/CaM binding domain, pH 7.5, 30°C | Gallus gallus | |
| 0.00047 | - |
1D-myo-inositol 1,4,5-trisphosphate | recombinant mutant K268E catalytic/CaM binding domain, pH 7.5, 30°C | Gallus gallus | |
| 0.00054 | - |
1D-myo-inositol 1,4,5-trisphosphate | recombinant mutant K272D catalytic/CaM binding domain, pH 7.5, 30°C | Gallus gallus | |
| 0.0017 | - |
1D-myo-inositol 1,4,5-trisphosphate | recombinant catalytic binding domain, pH 7.5, 30°C | Rattus norvegicus | |
| 0.033 | - |
ATP | recombinant catalytic/CaM binding domain, pH 7.5, 30°C | Rattus norvegicus | |
| 0.042 | - |
ATP | recombinant catalytic domain, pH 7.5, 30°C | Rattus norvegicus | |
| 0.074 | - |
ATP | recombinant wild-type catalytic/CaM binding domain, pH 7.5, 30°C | Gallus gallus | |
| 0.085 | - |
ATP | recombinant mutant K268E catalytic/CaM binding domain, pH 7.5, 30°C | Gallus gallus | |
| 0.105 | - |
ATP | recombinant mutant K272D catalytic/CaM binding domain, pH 7.5, 30°C | Gallus gallus | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Ca2+ | - |
Gallus gallus | |
| Ca2+ | - |
Homo sapiens | |
| Ca2+ | - |
Rattus norvegicus | |
| Mg2+ | - |
Gallus gallus | |
| Mg2+ | - |
Homo sapiens | |
| Mg2+ | - |
Rattus norvegicus | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + 1D-myo-inositol 1,4,5-trisphosphate | Gallus gallus | - |
ADP + 1D-myo-inositol 1,3,4,5-tetrakisphosphate | - |
? | |
| ATP + 1D-myo-inositol 1,4,5-trisphosphate | Homo sapiens | - |
ADP + 1D-myo-inositol 1,3,4,5-tetrakisphosphate | - |
? | |
| ATP + 1D-myo-inositol 1,4,5-trisphosphate | Rattus norvegicus | - |
ADP + 1D-myo-inositol 1,3,4,5-tetrakisphosphate | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Gallus gallus | - |
isozyme IP3K-A | - |
| Homo sapiens | - |
isozyme IP3K-A and IP3K-B | - |
| Rattus norvegicus | - |
isozyme IP3K-C | - |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| recombinant wild-type or mutant fragments comprising the catalytic domain and the CaM binding domain of isozyme IP3K-A and IP3K-B from Escherichia coli strain BL21(DE3) by phosphocellulose and CaM affinity chromatography | Homo sapiens |
| recombinant wild-type or mutant fragments comprising the catalytic domain and the CaM binding domain of isozyme IP3K-A from Escherichia coli strain BL21(DE3) by phosphocellulose and CaM affinity chromatography | Gallus gallus |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| erythrocyte | - |
Gallus gallus | - |
Specific Activity [micromol/min/mg]
| Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|
| 3 | - |
purified recombinant catalytic/CaM binding domain | Rattus norvegicus |
| 14 | - |
purified recombinant K268E catalytic/CaM binding domain | Gallus gallus |
| 15 | - |
purified recombinant wild-type catalytic/CaM binding domain | Gallus gallus |
| 16 | - |
purified catalytic binding domain | Rattus norvegicus |
| 16 | - |
purified recombinant K272D catalytic/CaM binding domain | Gallus gallus |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + 1D-myo-inositol 1,4,5-trisphosphate | - |
Gallus gallus | ADP + 1D-myo-inositol 1,3,4,5-tetrakisphosphate | - |
? | |
| ATP + 1D-myo-inositol 1,4,5-trisphosphate | - |
Homo sapiens | ADP + 1D-myo-inositol 1,3,4,5-tetrakisphosphate | - |
? | |
| ATP + 1D-myo-inositol 1,4,5-trisphosphate | - |
Rattus norvegicus | ADP + 1D-myo-inositol 1,3,4,5-tetrakisphosphate | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| inositol-1,4,5-trisphosphate 3-kinase | - |
Gallus gallus |
| inositol-1,4,5-trisphosphate 3-kinase | - |
Homo sapiens |
| inositol-1,4,5-trisphosphate 3-kinase | - |
Rattus norvegicus |
| IP3K | - |
Gallus gallus |
| IP3K | - |
Homo sapiens |
| IP3K | - |
Rattus norvegicus |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 30 | - |
assay at | Gallus gallus |
| 30 | - |
assay at | Homo sapiens |
| 30 | - |
assay at | Rattus norvegicus |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.5 | - |
assay at | Gallus gallus |
| 7.5 | - |
assay at | Homo sapiens |
| 7.5 | - |
assay at | Rattus norvegicus |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Gallus gallus | |
| ATP | - |
Homo sapiens | |
| ATP | - |
Rattus norvegicus | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | dose-response curve of antiproliferative synthetic and plant polyphenolics inhibition | Gallus gallus |
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