期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 203, 期 -, 页码 -出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2020.112571
关键词
Cancer; CDK inhibitors; Covalent inhibitors; Anticancer hybrids; Transcriptional CDKs; PROTACs
资金
- Department of Biotechnology (DBT), India Project [BT/PR16249/NER/95/105/2015]
- University Grant Commision (UGC), India [F.20-41/2013(BSR)]
- Department of Science and Technology (DST) [160764]
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.
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