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CDK inhibitor : ウィキペディア英語版
CDK inhibitor

A CDK (Cyclin-dependent kinase) inhibitor is a chemical that inhibits the function of CDKs. It is used to treat cancers by preventing overproliferation of cancer cells. The FDA has stated approving the first drugs now which is Ibrance, a CDK 4/6 inhibitor allowed for use in postmenopausal women with breast cancer that is ER positive and HER2 negative, several compounds are on clinical trials now (2009).
==CDKs as cancer target==
In many human cancers, CDKs are overactive or CDK-inhibiting proteins are not functional.〔Malumbres, M., and Barbacid, M. (2001). To cycle or not to cycle: a critical decision in cancer. Nature reviews 1, 222-231.〕〔Malumbres, M., and Barbacid, M. (2009). Cell cycle, CDKs and cancer: a changing paradigm. Nature reviews 9, 153-166.〕 Therefore, it is rational to target CDK function to prevent unregulated proliferation of cancer cells.

However, the validity of CDK as a cancer target should be carefully assessed because genetic studies have revealed that knockout of one specific type of CDK often does not affect proliferation of cells or has an effect only in specific tissue types. For example, most adult cells in mice proliferate normally even without both CDK4 and CDK2.〔Barriere, C., Santamaria, D., Cerqueira, A., Galan, J., Martin, A., Ortega, S., Malumbres, M., Dubus, P., and Barbacid, M. (2007). Mice thrive without Cdk4 and Cdk2. Molecular oncology 1, 72-83.〕
Furthermore, specific CDKs are only active in certain periods of the cell cycle. Therefore, the pharmacokinetics and dosing schedule of the candidate compound must be carefully evaulated to maintain active concentration of the drug throughout the entire cell cycle.〔Malumbres, M., Pevarello, P., Barbacid, M., and Bischoff, J.R. (2008). CDK inhibitors in cancer therapy: what is next? Trends in pharmacological sciences 29, 16-21.〕

抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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