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Literature summary extracted from

  • Chopra, P.; Sethi, G.; Dastidar, S.G.; Ray, A.
    Polo-like kinase inhibitors: an emerging opportunity for cancer therapeutics (2010), Expert Opin. Investig. Drugs, 19, 27-43.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.7.11.21 aurora A
-
 Homo sapiens
2.7.11.21 additional information activation of Plk1 requires phosphorylation of the conserved threonine residue Thr210 Homo sapiens

Application

EC Number Application Comment Organism
2.7.11.21 medicine Plk1 is a promising therapeutic target for the treatmment of cancer Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.21 5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3-[2-(trifluoromethyl)-benzyloxy]-thiophene-2-carboxamide
-
 Homo sapiens
2.7.11.21 BI2536
-
 Homo sapiens
2.7.11.21 BI6727
-
 Homo sapiens
2.7.11.21 GSK461364A
-
 Homo sapiens
2.7.11.21 HMN-214
-
 Homo sapiens
2.7.11.21 LY294002
-
 Homo sapiens
2.7.11.21 morin
-
 Homo sapiens
2.7.11.21 ON01910.Na
-
 Homo sapiens
2.7.11.21 quercetin
-
 Homo sapiens
2.7.11.21 SBE13
-
 Homo sapiens
2.7.11.21 scytonemin
-
 Homo sapiens
2.7.11.21 siRNA
-
 Homo sapiens
2.7.11.21 Wortmannin
-
 Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.7.11.21 centrosome
-
 Homo sapiens 5813
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.21 ATP + a protein Homo sapiens
-
 ADP + a phosphoprotein
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.21 Homo sapiens
-
-
-

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
2.7.11.21 phosphoprotein
-
 Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.21 breast
-
 Homo sapiens
-
2.7.11.21 colon
-
 Homo sapiens
-
2.7.11.21 lung
-
 Homo sapiens
-
2.7.11.21 ovary
-
 Homo sapiens
-
2.7.11.21 pancreas
-
 Homo sapiens
-
2.7.11.21 prostate
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.21 ATP + a protein
-
 Homo sapiens ADP + a phosphoprotein
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.11.21 Plk1
-
 Homo sapiens
2.7.11.21 polo-like kinase
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.21 ATP
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.11.21 0.00000005
-
 less than 50 nM Homo sapiens GSK461364A
2.7.11.21 0.0000008
-
-
 Homo sapiens BI2536
2.7.11.21 0.00000087
-
-
 Homo sapiens BI6727
2.7.11.21 0.000024
-
-
 Homo sapiens Wortmannin
2.7.11.21 0.00525
-
-
 Homo sapiens LY294002
2.7.11.21 0.0126
-
-
 Homo sapiens morin
2.7.11.21 0.064
-
-
 Homo sapiens quercetin

Expression

EC Number Organism Comment Expression
2.7.11.21 Homo sapiens Plk1 is overexpressed in tumors up

General Information

EC Number General Information Comment Organism
2.7.11.21 physiological function Plk1 is involved in the activation of Cdc2, chromosome segregation, centrosome maturation, bipolar spindle formation and execution of cytokinesis Homo sapiens