Cyclin dependent kinase (CDK) inhibitors as anticancer drugs

被引:208
|
作者
Sanchez-Martinez, Concepcion [1 ]
Gelbert, Lawrence M. [2 ]
Jose Lallena, Maria [1 ]
de Dios, Alfonso [3 ]
机构
[1] Eli Lilly & Co, Discovery Chem Res & Technol, Alcobendas 28108, Madrid, Spain
[2] Indiana Univ, Herman B Wells Ctr Pediat Res, Sect Pediat Hematol Oncol, Indianapolis, IN 46202 USA
[3] Eli Lilly & Co, Discovery Chem Res & Technol, Indianapolis, IN 46285 USA
关键词
CDK inhibitors; Cell cycle; CELL-CYCLE; ANTITUMOR-ACTIVITY; CANCER-THERAPY; IN-VITRO; POTENT; DISCOVERY; COMBINATION; IDENTIFICATION; OPTIMIZATION; PEPTIDES;
D O I
10.1016/j.bmcl.2015.05.100
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Sustained proliferative capacity is a hallmark of cancer. In mammalian cells proliferation is controlled by the cell cycle, where cyclin-dependent kinases (CDKs) regulate critical checkpoints. CDK4 and CDK6 are considered highly validated anticancer drug targets due to their essential role regulating cell cycle progression at the G1 restriction point. This review provides an overview of recent advances on cyclin dependent kinase inhibitors in general with special emphasis on CDK4 and CDK6 inhibitors and compounds under clinical evaluation. Chemical structures, structure activity relationships, and relevant preclinical properties will be described. (C) 2015 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3420 / 3435
页数:16
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