JZUS - Journal of Zhejiang University SCIENCE

Journal of Zhejiang University SCIENCE B

Accepted manuscript available online (unedited version)

Exploiting targeted degradation of cyclins and cyclin-dependent kinases for cancer thera-peutics: a review

Author(s): Suya ZHENG^1, ^2, ³, Ye CHEN^1, ^2, ⁴, Zhipeng ZHU³, Nan LI^1, ^2, ³, Chunyu HE³, H. Phillip KOEF-FLER⁵, Xin HAN⁶, Qichun WEI^7, ⁸, Liang XU^3, ^4, ⁷
Affiliation(s): ¹Department of Surgical Oncology, Children's Hospital Zhejiang University School of Medicine, Hangzhou 310052, China; more
Corresponding email(s): xinhan@zju.edu.cn, qichun_wei@zju.edu.cn, xuliang.phd@zju.edu.cn
Key Words: Cyclin-dependent kinase (CDK); Cyclin; Protein degrader; Targeted protein degradation

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Suya ZHENG^1,^2,³, Ye CHEN^1,^2,⁴, Zhipeng ZHU³, Nan LI^1,^2,³, Chunyu HE³, H. Phillip KOEF-FLER⁵, Xin HAN⁶, Qichun WEI^7,⁸, Liang XU^3,^4,⁷. Exploiting targeted degradation of cyclins and cyclin-dependent kinases for cancer thera-peutics: a review[J]. Journal of Zhejiang University Science B,in press.Frontiers of Information Technology & Electronic Engineering,in press.https://doi.org/10.1631/jzus.B2500021

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author="Suya ZHENG^1,^2,³, Ye CHEN^1,^2,⁴, Zhipeng ZHU³, Nan LI^1,^2,³, Chunyu HE³, H. Phillip KOEF-FLER⁵, Xin HAN⁶, Qichun WEI^7,⁸, Liang XU^3,^4,⁷",
journal="Journal of Zhejiang University Science B",
year="in press",
publisher="Zhejiang University Press & Springer",
doi="https://doi.org/10.1631/jzus.B2500021"
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Abstract
Chinese Summary
Academic Network
Reviewer Comment

Abstract: Cancer is characterized by abnormal cell proliferation. Cyclins and cyclin-dependent kinases (CDKs) have been recognized as essential regulators of the intricate cell cycle, orchestrating DNA replication, transcription, RNA splicing, and protein synthesis. Dysregulation of the CDK pathway is prevalent in the development and progression of human cancers, rendering cyclins and CDKs attractive therapeutic targets. Several CDK4/6 inhibitors have demonstrated promising anti-cancer efficacy and have been successfully translated into clinical use, fueling the development of CDK-targeted therapies. With this enthusiasm for finding novel CDK-targeting anti-cancer agents, there have also been exciting advances in the field of targeted protein degradation through innovative strategies, such as using proteolysis-targeting chimera, HSP90-mediated targeting chimera, hydrophobic tag-based protein degradation, and molecular glue. With a focus on the translational potential of cyclin- and CDK-targeting strategies in cancer, this review presents the fundamental roles of cyclins and CDKs in cancer. Furthermore, it summarizes current strategies for the proteasome-dependent targeted degradation of cyclins and CDKs, detailing the underlying mechanisms of action for each approach. A comprehensive overview of the structure and activity of existing CDK degraders is also provided. By examining the structure-activity relationships, target profiles and biological effects of reported cyclin/CDK degraders, this review provides a valuable reference for both CDK pathway-targeted biomedical research and cancer therapeutics.

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