Cyclin dependent kinase (CDK) inhibitors as anticancer drugs
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs
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DOI：
10.1016/j.bmcl.2015.05.100
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发表时间：
2015-09-01
影响因子：
2.7
通讯作者：
de Dios, Alfonso
中科院分区：
文献类型：
--
作者：
Sanchez-Martinez, Concepcion;Gelbert, Lawrence M.;de Dios, Alfonso
持续的增殖能力是癌症的标志。在哺乳动物细胞中，增殖受细胞周期控制，其中细胞周期蛋白依赖性激酶（CDK）调节关键检查点。CDK4和CDK6被认为是高度验证的抗癌药物靶点，因为它们在G1限制点调节细胞周期进展的重要作用。本文综述了细胞周期蛋白依赖性激酶抑制剂的最新进展，特别强调了CDK4和CDK6抑制剂和正在进行临床评价的化合物。将描述化学结构、构效关系和相关临床前性质。(C)2015爱思唯尔有限公司版权所有。
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.