Target Validation Information | |||||
---|---|---|---|---|---|
Target ID | T89361 | ||||
Target Name | Cell division protein kinase 6 | ||||
Target Type | Successful |
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Drug Potency against Target | PD-332991 | Drug Info | Ki = 15 nM | [552469] | |
Flavopiridol | Drug Info | IC50 = 60 nM | [537564] | ||
FISETIN | Drug Info | IC50 = 850 nM | [527422] | ||
CHRYSIN | Drug Info | IC50 = 6000 nM | [527422] | ||
APIGENIN | Drug Info | IC50 = 1700 nM | [527422] | ||
Action against Disease Model | PD-332991 | Inhibited cellular proliferation with IC50 = 40-400 nM in RB1-positive cell lines and IC50 > 3 mM in RB1-negative cell lines; induced G1 arrest in primary bone marrow myeloma cells and prevented t uMour growth in disseminated h uMan myeloma xenografts; promoted t uMour regression in mice with a h uMan colon carcinoma xenograft. | [537564] | Drug Info | |
The Effect of Target Knockout, Knockdown or Genetic Variations | In unstressed thymocytes, CDK6 kinase activity is lost in CDK6 KO animals; the thymic defects observed in the KO animals are the result of changes in CDK6 protein level resulting from the presence of the LSL cassette; CDK6 loss interferes with the proliferation and survival signals instigated by Notch signaling.Further,those thymocytes that survive CDK6 loss display defects in maturation consistent with a role for CDK6 in potentiating early stages and inhibiting late stages of Notch-regulated differentiation. | [552469] | |||
References | |||||
Ref 552469 | Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther. 2004 Nov;3(11):1427-38. | ||||
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 527422 | J Med Chem. 2005 Feb 10;48(3):737-43.Crystal structure of a human cyclin-dependent kinase 6 complex with a flavonol inhibitor, fisetin. | ||||
Ref 527422 | J Med Chem. 2005 Feb 10;48(3):737-43.Crystal structure of a human cyclin-dependent kinase 6 complex with a flavonol inhibitor, fisetin. | ||||
Ref 527422 | J Med Chem. 2005 Feb 10;48(3):737-43.Crystal structure of a human cyclin-dependent kinase 6 complex with a flavonol inhibitor, fisetin. |
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