A comprehensive insight on the recent development of Cyclic Dependent Kinase inhibitors as anticancer agents

被引：35

作者：

Marak, Brilliant N. ^{[1
]}

Dowarah, Jayanta ^{[1
]}

Khiangte, Laldingluaia ^{[1
]}

Singh, Ved Prakash ^{[1
]}

机构：

[1] Mizoram Univ, Sch Phys Sci, Dept Chem, Aizawl 796004, Mizoram, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2020年 / 203卷

关键词：

Cancer; CDK inhibitors; Covalent inhibitors; Anticancer hybrids; Transcriptional CDKs; PROTACs; CDK8/19 DUAL INHIBITORS; BIOLOGICAL EVALUATION; HIGHLY POTENT; ANTITUMOR-ACTIVITY; CDK INHIBITORS; SELECTIVE INHIBITORS; THERAPEUTIC TARGETS; MOLECULAR DOCKING; STRUCTURAL BASIS; DISCOVERY;

D O I：

10.1016/j.ejmech.2020.112571

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Cancer is one of the major leading causes of death worldwide despite many breakthroughs in the development of novel anticancer drugs. The heterodimer CDK-Cyclin complex plays an essential role in regulating cellular processes. For example, epigenetics, neuronal activity, gene transcription, metabolism, DNA repair, angiogenesis, and hematopoiesis. Consequently, CDKs are often deregulated and over-expressed, causing an uncontrolled proliferation in tumors. Due to their active role in cell cycle regulation and transcription activity, CDKs are conceived as promising targets to overcome cell proliferation. Therefore, designing and developing efficient Cyclic Dependent Kinase inhibitors is progressively becoming a credible solution in treating cancers. This review article emphasized the recent developments of cyclic dependent Kinase inhibitors with insights into their structure-activity relationship, molecular docking, and mechanism of action. (C) 2020 Elsevier Masson SAS. All rights reserved.

引用

页数：46

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