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Updated: Sep 19, 2025

High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines
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Research Progress of PROTAC-Degraded CDKs in the Treatment of Breast Cancer

Kexin Zhao1, Jun Zhang1, Zhe Yang1

  • 1Yan'an Medical College of Yan'an University, Yan'an, People's Republic of China.

Breast Cancer (Dove Medical Press)
|June 19, 2025
PubMed

Insights

PROteolysis Targeting Chimeras (PROTACs) offer a novel approach to breast cancer treatment by degrading cyclin-dependent protein kinases (CDKs). This targeted protein degradation inhibits cancer cell proliferation, presenting a promising therapeutic strategy.

Area of Science:

  • Oncology
  • Molecular Biology
  • Biochemistry

Background:

  • Breast cancer (BC) is a leading cause of cancer-related deaths globally, primarily affecting women.
  • Cyclin-dependent protein kinases (CDKs) are frequently dysregulated in breast cancer, impacting cell cycle progression.
  • Specific CDKs like CDK4/6, CDK1, and CDK12 play critical roles in breast cancer development and progression.

Purpose of the Study:

  • To review the role of cyclin-dependent protein kinases (CDKs) in breast cancer.
  • To explore the potential of PROteolysis Targeting Chimeras (PROTACs) in targeting CDKs for breast cancer therapy.
  • To summarize research on PROTAC-mediated degradation of CDKs as a novel therapeutic strategy.

Main Methods:

  • Literature review of studies on CDKs in breast cancer.
  • Review of PROteolysis Targeting Chimeras (PROTACs) technology for targeted protein degradation.
  • Analysis of PROTACs' mechanism in ubiquitin-proteasome mediated degradation of CDKs.

Main Results:

  • High expression or dysregulation of CDKs is strongly associated with breast cancer.
  • PROTACs can effectively induce ubiquitination and proteasomal degradation of key CDKs (CDK1, CDK4/6, CDK9, CDK12/13).
  • PROTAC-mediated degradation of CDKs inhibits breast cancer cell proliferation.

Conclusions:

  • PROTAC technology demonstrates significant potential for targeting CDK dysregulation in breast cancer.
  • PROTACs represent a promising novel therapeutic approach for breast cancer treatment.
  • Targeted degradation of CDKs via PROTACs offers a new avenue for combating breast cancer.
Keywords:
CDKsPROTACbreast cancerubiquitin

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