Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.
Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy.
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DOI：
10.1021/acs.jmedchem.6b00150
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发表时间：
2016-10-13
影响因子：
7.3
通讯作者：
Natarajan A
中科院分区：
文献类型：
--
作者：
Sonawane YA;Taylor MA;Napoleon JV;Rana S;Contreras JI;Natarajan A
细胞周期蛋白依赖性激酶(CDK)抑制剂因其在细胞内的广泛而关键的功能而成为近20年来研究的热点。最近，CDK9已成为癌症治疗发展的可用药靶点。CDK9在转录调控中起着至关重要的作用，尤其是CDK9介导的对短命抗凋亡蛋白的转录调控对转化细胞的生存至关重要。在选择性CDK9抑制剂的开发方面，基于过多支架的集中化学库取得了好坏参半的结果。在这里，我们综述了CDK9的调控，它的细胞功能，用于靶向CDK9的常见核心结构，以及它们在体外和体内的选择性和有效性。
Cyclin dependent kinase (CDK) inhibitors have been the topic of intense research for nearly 2 decades due to their widely varied and critical functions within the cell. Recently CDK9 has emerged as a druggable target for the development of cancer therapeutics. CDK9 plays a crucial role in transcription regulation; specifically, CDK9 mediated transcriptional regulation of short-lived antiapoptotic proteins is critical for the survival of transformed cells. Focused chemical libraries based on a plethora of scaffolds have resulted in mixed success with regard to the development of selective CDK9 inhibitors. Here we review the regulation of CDK9, its cellular functions, and common core structures used to target CDK9, along with their selectivity profile and efficacy in vitro and in vivo.
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影响因子：
4
作者：
Baumli S;Hole AJ;Noble ME;Endicott JA
通讯作者：
Endicott JA
影响因子：
46.9
作者：
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--
影响因子：
11.4
作者：
Baumli, Sonja;Lolli, Graziano;Johnson, Louise N.
通讯作者：
Johnson, Louise N.
影响因子：
3.2
作者：
Ali, Akbar;Ghosh, Animesh;Rana, Tariq M.
通讯作者：
Rana, Tariq M.
影响因子：
6.1
作者：
Bose P;Simmons GL;Grant S
通讯作者：
Grant S