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 534283Br 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 528764J Biol Chem. 2007 May 18;282(20):14845-52. Epub 2007 Mar 28.Cellular characterization of a novel focal adhesion kinase inhibitor.
Ref 537564Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
Ref 537564Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
Ref 553081A 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 537564Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
Ref 537564Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.

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