CDK抑制剂在抗肿瘤领域的研发进展  

Progress in Development of Cyclin-dependent Kinase Inhibitors as Cancer Therapy

作　　者：谢韶 丁健[1] 陈奕[1] 

机构地区：[1]中国科学院上海药物研究所新药研究国家重点实验室肿瘤药理组,上海201203

出　　处：《药学进展》2015年第10期734-745,共12页Progress in Pharmaceutical Sciences

摘　　要：细胞周期蛋白依赖性激酶(cyclindependentkinase,CDK)为细胞周期调节的关键激酶,参与细胞增殖、转录、存活等生理过程。CDK在多种肿瘤中异常活化,是抗肿瘤药物研发的重要靶点之一。目前已有1个CDK抑制剂(palbociclib,CDK4/CDK6抑制剂)被美国食品药品监督管理局批准于2015年上市,数十个CDK抑制剂处于针对实体瘤和血液系统肿瘤的临床或临床前研究阶段。综述目前抗肿瘤领域CDK抑制剂的研发现状、遇到的问题和可能的解决方案,并讨论其临床应用的可能。Cyclin-dependent kinases（CDKs） play critical roles in controlling cell cycle and regulating cell proliferation, transcription and survival. CDKs are often abnormally activated in numerous tumors and thus become attractive anticancer targets. Palbociclib, a CDK4/CDK6 inhibitor, was approved by the US Food and Drugs Administration in 2015, Dozens of compounds targeting CDKs are currently in clinical development for various solid tumors and hematopoietic malignances.In this article, the recent studies on CDK inhibitors, related challenges and solutions were reviewed, and the probable clinical application of CDK inhibitors was also discussed.

关 键 词：CDK 抑制剂 ATP竞争 非ATP竞争 联合用药 

分 类 号：R96[医药卫生—药理学]