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Literature summary for 2.7.11.22 extracted from
- Determination of kinetic parameters and structure-activity relationships of ginsenosides as inhibitors of cyclin-dependent kinase 5/p25 using ultra-pressure liquid chromatography with triple quadrupole tandem mass spectrometry (2013), Rapid Commun. Mass Spectrom., 27, 985-992.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| p25 | required for activity | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| ginsenoside F1 | noncompetitive inhibition | Homo sapiens |  |
| ginsenoside Rb1 | noncompetitive inhibition | Homo sapiens | |
| ginsenoside Re | noncompetitive inhibition | Homo sapiens | |
| ginsenoside Rf | noncompetitive inhibition | Homo sapiens | |
| ginsenoside Rg1 | noncompetitive inhibition | Homo sapiens | |
| ginsenoside Rg2 | noncompetitive inhibition | Homo sapiens | |
| ginsenoside Rh1 | noncompetitive inhibition | Homo sapiens | |
| additional information | ginsenosides as inhibitors of cyclin-dependent kinase 5/p25, structure-activity relationships, overview. Ginsenosides Rd, F2, Rb3, Rb2, Rg3, Rc, and Rh2 are no inhibitors of Cdk5/p25. No inhibition by protopanaxadiol | Homo sapiens | |
| protopanaxatriol | noncompetitive inhibition | Homo sapiens | |
| roscovitine | competitive inhibitor | Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.00285 | - |
PKTPKKAKKL | pH 7.5, 37°C | Homo sapiens | |
| 0.00522 | - |
ATP | pH 7.5, 37°C | Homo sapiens | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | required | Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| commercial preparation | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + PKTPKKAKKL | - |
Homo sapiens | ADP + PKpTPKKAKKL | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| Cdk5 | - |
Homo sapiens |
| cyclin-dependent kinase 5 | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 30 | 37 | assay at | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.5 | - |
- |
Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.00025 | - |
pH 7.5, 37°C | Homo sapiens | roscovitine | |
| 0.00431 | - |
pH 7.5, 37°C | Homo sapiens | protopanaxatriol | |
| 0.0069 | - |
pH 7.5, 37°C | Homo sapiens | ginsenoside F1 | |
| 0.00728 | - |
pH 7.5, 37°C | Homo sapiens | ginsenoside Rh1 | |
| 0.00785 | - |
pH 7.5, 37°C | Homo sapiens | ginsenoside Rg1 | |
| 0.00901 | - |
pH 7.5, 37°C | Homo sapiens | ginsenoside Re | |
| 0.00976 | - |
pH 7.5, 37°C | Homo sapiens | ginsenoside Rf | |
| 0.0108 | - |
pH 7.5, 37°C | Homo sapiens | ginsenoside Rg2 | |
| 0.02496 | - |
pH 7.5, 37°C | Homo sapiens | ginsenoside Rb1 | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| additional information | effect of ginsenosides on Alzheimer's disease may be involved with the regulation of activities of cdk5/p25. Enzyme activity measurement by mass spectrometry, UPLC/TQMS method development, usage with liquid chromatographic separation of product, overview | Homo sapiens |
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