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Recent Progress in CDK4/6 Inhibitors and PROTACs.

ABSTRACT: Cell division in eukaryotes is a highly regulated process that is critical to the life of a cell. Dysregulated cell proliferation, often driven by anomalies in cell Cyclin-dependent kinase (CDK) activation, is a key pathological mechanism in cancer. Recently, selective CDK4/6 inhibitors have shown clinical success, particularly in treating advanced-stage estrogen receptor (ER)-positive and human epidermal growth factor receptor 2 (HER2)-negative breast cancer. This review provides an in-depth analysis of the action mechanism and recent advancements in CDK4/6 inhibitors, categorizing them based on their structural characteristics and origins. Furthermore, it explores proteolysis targeting chimers (PROTACs) targeting CDK4/6. We hope that this review could be of benefit for further research on CDK4/6 inhibitors and PROTACs.

SUBMITTER: Wang H

PROVIDER: S-EPMC10745860 | biostudies-literature | 2023 Dec

REPOSITORIES: biostudies-literature

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Recent Progress in CDK4/6 Inhibitors and PROTACs.

Wang Hao H Ba Jianfei J Kang Yue Y Gong Zeqiao Z Liang Tingting T Zhang Yahong Y Qi Jianguo J Wang Jianhong J

Molecules (Basel, Switzerland) 20231213 24

Cell division in eukaryotes is a highly regulated process that is critical to the life of a cell. Dysregulated cell proliferation, often driven by anomalies in cell Cyclin-dependent kinase (CDK) activation, is a key pathological mechanism in cancer. Recently, selective CDK4/6 inhibitors have shown clinical success, particularly in treating advanced-stage estrogen receptor (ER)-positive and human epidermal growth factor receptor 2 (HER2)-negative breast cancer. This review provides an in-depth an ...[more]

PMID: 38138549

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