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Literature summary for 2.7.11.21 extracted from
- Polo-like kinase inhibitors: an emerging opportunity for cancer therapeutics (2010), Expert Opin. Investig. Drugs, 19, 27-43.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| aurora A | - |
Homo sapiens | |
| additional information | activation of Plk1 requires phosphorylation of the conserved threonine residue Thr210 | Homo sapiens |
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | Plk1 is a promising therapeutic target for the treatmment of cancer | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3-[2-(trifluoromethyl)-benzyloxy]-thiophene-2-carboxamide | - |
Homo sapiens |  |
| BI2536 | - |
Homo sapiens | |
| BI6727 | - |
Homo sapiens | |
| GSK461364A | - |
Homo sapiens | |
| HMN-214 | - |
Homo sapiens | |
| LY294002 | - |
Homo sapiens | |
| morin | - |
Homo sapiens | |
| ON01910.Na | - |
Homo sapiens | |
| quercetin | - |
Homo sapiens | |
| SBE13 | - |
Homo sapiens | |
| scytonemin | - |
Homo sapiens | |
| siRNA | - |
Homo sapiens | |
| Wortmannin | - |
Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| centrosome | - |
Homo sapiens | 5813 | - |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + a protein | Homo sapiens | - |
ADP + a phosphoprotein | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Posttranslational Modification
| Posttranslational Modification | Comment | Organism |
|---|---|---|
| phosphoprotein | - |
Homo sapiens |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| breast | - |
Homo sapiens | - |
| colon | - |
Homo sapiens | - |
| lung | - |
Homo sapiens | - |
| ovary | - |
Homo sapiens | - |
| pancreas | - |
Homo sapiens | - |
| prostate | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + a protein | - |
Homo sapiens | ADP + a phosphoprotein | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| Plk1 | - |
Homo sapiens |
| polo-like kinase | - |
Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.00000005 | - |
less than 50 nM | Homo sapiens | GSK461364A | |
| 0.0000008 | - |
- |
Homo sapiens | BI2536 | |
| 0.00000087 | - |
- |
Homo sapiens | BI6727 | |
| 0.000024 | - |
- |
Homo sapiens | Wortmannin | |
| 0.00525 | - |
- |
Homo sapiens | LY294002 | |
| 0.0126 | - |
- |
Homo sapiens | morin | |
| 0.064 | - |
- |
Homo sapiens | quercetin | |
Expression
| Organism | Comment | Expression |
|---|---|---|
| Homo sapiens | Plk1 is overexpressed in tumors | up |
General Information
| General Information | Comment | Organism |
|---|---|---|
| physiological function | Plk1 is involved in the activation of Cdc2, chromosome segregation, centrosome maturation, bipolar spindle formation and execution of cytokinesis | Homo sapiens |
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