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细胞周期蛋白依赖性激酶 9(CDK9)作为药物靶点的展望。

Perspective of cyclin-dependent kinase 9 (CDK9) as a drug target.

机构信息

Laboratory of Growth Regulators, Palacký University, Šlechtitelů 11, 78371, Olomouc, Czech Republic.

出版信息

Curr Pharm Des. 2012;18(20):2883-90. doi: 10.2174/138161212800672750.

Abstract

Deregulation of cyclin-dependent kinases (CDKs) has been associated with many cancer types and has evoked an interest in chemical inhibitors with possible therapeutic benefit. While most known inhibitors display broad selectivity towards multiple CDKs, recent work highlights CDK9 as the critical target responsible for the anticancer activity of clinically evaluated drugs. In this review, we discuss recent findings provided by structural biologists that may allow further development of highly specific inhibitors of CDK9 towards applications in cancer therapy. We also highlight the role of CDK9 in inflammatory processes and diseases.

摘要

细胞周期蛋白依赖性激酶(CDKs)的失调与许多癌症类型有关,并引起了人们对具有潜在治疗益处的化学抑制剂的兴趣。虽然大多数已知的抑制剂对多种 CDK 表现出广泛的选择性,但最近的工作强调 CDK9 是负责临床评估药物抗癌活性的关键靶标。在这篇综述中,我们讨论了结构生物学家提供的最新发现,这些发现可能有助于进一步开发针对 CDK9 的高度特异性抑制剂,以应用于癌症治疗。我们还强调了 CDK9 在炎症过程和疾病中的作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/afb5/3382371/c6bb2abf42ec/CPD-18-2883_F1.jpg

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