Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy,Journal of Medicinal Chemistry

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Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2016-06-03 00:00:00 , DOI: 10.1021/acs.jmedchem.6b00150
Yogesh A. Sonawane ₁ , Margaret A. Taylor ₁ , John Victor Napoleon ₁ , Sandeep Rana ₁ , Jacob I. Contreras ₁ , Amarnath Natarajan ₁

Affiliation

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.

中文翻译：

细胞周期蛋白依赖性激酶9抑制剂用于癌症治疗

细胞周期蛋白依赖性激酶（CDK）抑制剂由于其在细胞内的广泛变化和关键功能而成为近20年的研究热点。最近，CDK9已经成为开发癌症治疗药物的可治疗靶标。CDK9在转录调控中起着至关重要的作用。具体而言，CDK9介导的短寿抗凋亡蛋白的转录调控对于转化细胞的存活至关重要。基于大量支架的聚焦化学文库在开发选择性CDK9抑制剂方面取得了成功的混合结果。在这里，我们回顾了CDK9的调节，其细胞功能以及用于靶向CDK9的常见核心结构，以及它们在体外和体内的选择性和功效。

更新日期：2016-06-03

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