期刊
RSC ADVANCES
卷 11, 期 47, 页码 29227-29246出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/d1ra03820f
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资金
- JSS Academy of Higher Education & Research, Mysuru, Karnataka, India
The discovery of CDK4/6 inhibitors is considered a game-changer in cancer therapy, as their inhibition triggers cell cycle arrest and apoptosis. Targeting CDK4/6 has been proposed as a paradigm shift in anticancer approaches, and the development of effective inhibitors is becoming a promising cancer therapy.
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.
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