Discovery and Development of Cyclin-Dependent Kinase 8 Inhibitors

Author:

Lv Xiao1,Tian Yongbing1,Li Shiyu1,Cheng Kai1,Huang Xufeng1,Kong Haiyan1,Liao Chenzhong1,Xie Zhouling1

Affiliation:

1. School of Food and Biological Engineering, Hefei University of Technology, Hefei, Anhui 230009, China

Abstract

Cyclin-dependent Kinase 8 (CDK8), a member of the CDKs family, has been widely focused owing to investigations of its critical roles in transcription and oncogenesis in recent years. Selective inhibition of CDK8 and its paralog CDK19 offers a novel therapeutic strategy for the treatment of some cancers. Up to now, though many small molecules against CDK8 have been discovered, most of them are discontinued in the preclinical trials due to the low selectivity and poor physicochemical properties. This review mainly summarizes the design strategies of selective CDK8 inhibitors having different chemical scaffolds with the aim to improve the inhibitory activity, selectivity, metabolic stability and solubility. Their corresponding Structure-activity Relationships (SAR) are also reviewed. On the basis of the discussion in this review, we hope more effective, selective and drug-like CDK8 inhibitors will be developed and demonstrate therapeutic values in the near future.

Funder

Fundamental Research Funds for the Central Universities

National Natural Science Foundation of China

Publisher

Bentham Science Publishers Ltd.

Subject

Pharmacology,Molecular Medicine,Drug Discovery,Biochemistry,Organic Chemistry

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