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Literature summary for 2.7.11.22 extracted from
- Crystal structure of a human cyclin-dependent kinase 6 complex with a flavonol inhibitor, fisetin (2005), J. Med. Chem., 48, 737-743.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| p25 | regulatory subunit of Cdk5 | Homo sapiens |
Application
| Application | Comment | Organism |
|---|---|---|
| drug development | CDKs are important targets for the design of drug with antimitotic and antineurodegenerative effects | Homo sapiens |
Crystallization (Commentary)
| Crystallization (Comment) | Organism |
|---|---|
| CDK6/cyclin V in complex with flavonol inhibitor fisetin, X-ray diffraction structure determination and analysis at 2.9 A resolution, modeling | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| apigenin | a flavonoid inhibitor of CDK6, CDK5, and CDK1 | Homo sapiens |  |
| chrysin | a flavonoid inhibitor of CDK6, CDK5, and CDK1 | Homo sapiens | |
| fisetin | a flavonol inhibitor of CDK6, CDK5, and CDK1, binding structure with CDK6 involving V101, E61, K43, D163, and E99 of CDK6, overview | Homo sapiens | |
| flavopiridol | an effective flavonoid inhibitor of CDK6, CDK5, and CDK1 | Homo sapiens | |
| kaempferol | a less potent flavonoid inhibitor of CDK6, CDK5, and CDK1 | Homo sapiens | |
| luteolin | a flavonoid inhibitor of CDK5 and CDK1 | Homo sapiens | |
| additional information | structure-function relationship of flavonoid inhibitors, IC50 values, overview | Homo sapiens | |
| quercetin | a less potent flavonoid inhibitor of CDK6, CDK5, and CDK1 | Homo sapiens | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | - |
Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | Homo sapiens | the CDKs play a central role in cell cycle control, apoptosis, transcription, and neuronal functions | ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + histone H1 | - |
Homo sapiens | ADP + phosphorylated histone H1 | - |
? | |
| additional information | the CDKs play a central role in cell cycle control, apoptosis, transcription, and neuronal functions | Homo sapiens | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| Cdk1 | - |
Homo sapiens |
| Cdk5 | - |
Homo sapiens |
| cdk6 | - |
Homo sapiens |
| cyclin-dependent kinase 6 | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 30 | - |
assay at | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7 | - |
assay at | Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Homo sapiens | |
| cyclin B | regulatory subunit of CDK1 | Homo sapiens | |
| cyclin V | regulatory subunit of CDK6 | Homo sapiens |
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Release 2023.1 (January 2023)
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