Issue 47, 2021

CDK4/6 inhibitors: a brief overview and prospective research directions

Abstract

The discovery of cyclin-dependent kinases (CDK) and their mechanism in regulating the cell cycle process was considered a game-changer in cancer therapy. Cell cycle arrest and apoptosis were both triggered by their inhibition. The CDK4/6 complex acts as a checkpoint during the cell cycle transition from cell growth (G1) to DNA synthesis (S) phase and its deregulation or overexpression induces abnormal cell proliferation and cancer development. Consequently, targeting CDK4/6 has been proposed as a paradigm shift in the anticancer approach. The design and development of effective CDK4/6 inhibitors are increasingly becoming a promising cancer therapy evident with approved drugs such as palbociclib, ribociclib, and abemaciclib, etc. In this article, we explore the biological importance of CDK4/6 in cancer therapy, the development of resistance to monotherapy, and a short overview of PROTAC (Proteolysis Targeting Chimera), a unique and pioneering technique for degrading CDK4/6 enzymes. Overall, our prime focus is to discuss novel CDK4/6 inhibitors with diverse chemical classes and their correlation with computational studies.

Graphical abstract: CDK4/6 inhibitors: a brief overview and prospective research directions

Article information

Article type
Review Article
Submitted
16 Maijs 2021
Accepted
22 Aug. 2021
First published
01 Sept. 2021
This article is Open Access
Creative Commons BY-NC license

RSC Adv., 2021,11, 29227-29246

CDK4/6 inhibitors: a brief overview and prospective research directions

T. Adon, D. Shanmugarajan and H. Y. Kumar, RSC Adv., 2021, 11, 29227 DOI: 10.1039/D1RA03820F

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