Target Validation Information | |||||
---|---|---|---|---|---|
Target ID | T58449 | ||||
Target Name | Cell division protein kinase 7 | ||||
Target Type | Clinical Trial |
||||
Drug Potency against Target | SNS-032 | Drug Info | Ki = 62 nM | [534283] | |
PF-228 | Drug Info | IC50 = 197 nM | [528764] | ||
R547 | Drug Info | IC50 = 1~3 nM | [537564] | ||
2,5-dichloro-N-p-tolylthiophene-3-sulfonamide | Drug Info | IC50 = 800 nM | |||
R-roscovitine | Drug Info | Ki = 540 nM | [553081] | ||
ZK 304709 | Drug Info | IC50 = 85 nM | [537564] | ||
Flavopiridol | Drug Info | IC50 = 110~300 nM | [537564] | ||
Action against Disease Model | ZK 304709 | Blocked growth of h uMan t uMour cell lines at IC50 = 317 nM, by inducing a dose-dependent G1-S arrest followed by apoptosis. Superior efficacy over standard chemotherapy in h uMan t uMour xenografts and orthotopic mouse models of h uMan pancreatic cancer. | [537564] | Drug Info | |
The Effect of Target Knockout, Knockdown or Genetic Variations | Using both Mat1(-/-) mouse embryonic fibroblasts and Cdk7 knockdown approaches, we show that the Cdk7 complex is an inhibitor of adipogenesis and is required for inactivation ofPPARgamma through the phosphorylation of PPARgamma-S112. The results demonstrate that the Cdk7 submodule of TFIIH acts as a physiological roadblock to adipogenesis by inhibiting PPARgamma activity. The observation that components of TFIIH are absent from transcriptionally active adipose tissue prompts a reevaluation of the ubiquitous nature of basal transcription factors in mammalian tissues. | [534283] | |||
References | |||||
Ref 534283 | Br J Pharmacol. 1996 Nov;119(6):1101-8.2-Amino-4-methylpyridine as a potent inhibitor of inducible NO synthase activity in vitro and in vivo. | ||||
Ref 528764 | J Biol Chem. 2007 May 18;282(20):14845-52. Epub 2007 Mar 28.Cellular characterization of a novel focal adhesion kinase inhibitor. | ||||
Ref 537564 | Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66. | ||||
Ref 537564 | Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66. | ||||
Ref 553081 | A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. J Med Chem. 2010 Dec 23;53(24):8508-22. doi: 10.1021/jm100732t. Epub 2010 Nov 16. | ||||
Ref 537564 | Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66. | ||||
Ref 537564 | Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66. |
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