Proteolysis Targeting Chimeras (PROTACs) in Breast Cancer Therapy

Yerim Jin1, Yeongju Lee1

  • 1Department of Chemistry, Pusan National University, Busan, 46241, Korea.

Chemmedchem
|August 13, 2024
PubMed

Insights

Proteolysis-targeting chimeras (PROTACs) offer a novel therapeutic strategy for breast cancer (BC) by degrading disease-causing proteins. This review explores current PROTAC developments, limitations, and future potential in BC treatment.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Breast cancer (BC) represents a significant global health challenge, comprising 30% of cancer cases in women worldwide.
  • The urgent need for selective and effective BC therapies drives research into innovative treatment modalities.
  • Proteolysis-targeting chimeras (PROTACs) have emerged as a promising therapeutic strategy for BC due to their unique mechanism of action.

Purpose of the Study:

  • To review the current landscape of PROTACs developed for targeting breast cancer.
  • To categorize existing PROTACs based on the specific types of breast cancer they target.
  • To discuss the limitations and future perspectives of PROTAC technology in the context of breast cancer therapeutics.

Main Methods:

  • Literature review of existing PROTAC molecules and their applications in breast cancer research.
  • Analysis of PROTAC design, including target protein ligands, E3 ligase ligands, and conjugating linkers.
  • Categorization of PROTACs based on breast cancer subtypes and targeted proteins.

Main Results:

  • PROTACs function by hijacking the cell's natural protein degradation machinery to eliminate target proteins.
  • This approach allows for the degradation of proteins previously considered undruggable, offering new therapeutic avenues.
  • Current PROTAC research demonstrates potential for high efficacy at low doses due to their catalytic nature.

Conclusions:

  • PROTACs represent a groundbreaking therapeutic strategy with significant potential for treating various types of breast cancer.
  • Further research is needed to overcome existing limitations and fully realize the clinical utility of PROTACs in BC treatment.
  • The review highlights the evolving role of PROTACs in precision oncology and their future prospects in combating breast cancer.