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Protacs Targeting ERα in the Effective Management of Endocrinal Resistance Breast Cancer

Anupriya Singh1, Roshni Khan1, Noora Amana Erachampatt1

  • 1Department of Pharmaceutical Sciences and Natural Products, School of Health Sciences, Central University of Punjab, Bathinda, Punjab, India.

Archiv Der Pharmazie
|December 23, 2025
PubMed

Insights

Proteolysis-targeting chimeras (PROTACs) offer a novel approach to degrade estrogen receptor alpha (ERα), addressing limitations of current therapies. This strategy shows promise for overcoming endocrine resistance in ERα-positive breast cancers.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Estrogen receptor alpha (ERα) is crucial for estrogen-driven gene expression and physiological processes.
  • Conventional endocrine therapies like SERMs and SERDs face challenges including acquired resistance and reduced efficacy in ERα-mutant cancers.

Purpose of the Study:

  • To review the mechanism of action, design, and application of Proteolysis-targeting chimeras (PROTACs) for degrading ERα.
  • To highlight structure-activity relationship (SAR) studies and in vitro/in vivo data for ERα-targeting PROTACs.

Main Methods:

  • Review of existing literature on PROTAC technology and ERα biology.
  • Analysis of SAR studies and experimental data for ERα-targeting PROTACs.
  • Discussion of strategies for designing effective ERα degraders.

Main Results:

  • PROTACs selectively and efficiently degrade ERα, offering a next-generation therapeutic strategy.
  • Elacestrant's approval has spurred interest in novel ERα degrader development.
  • Literature data provides insights into designing PROTACs with improved efficacy.

Conclusions:

  • PROTACs represent a promising therapeutic strategy to overcome endocrine resistance in ERα-positive breast cancers.
  • Further development of ERα-targeting PROTACs can advance treatment options for breast cancer patients.
Keywords:
ERαPROTACsSARSERDsbreast cancer

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