Development of PROTACs targeting estrogen receptor: an emerging technique for combating endocrine resistance

  • RSC Med Chem. 2024 Dec 30;16(3):1023-1036. doi: 10.1039/d4md00961d.
Rouming Peng  1 ,  Xin Liu  1 ,  Chun-Chi Chen  1  2 ,  Rey-Ting Guo  1  2 ,  Jian Min  1
Affiliations
  • 1. State Key Laboratory of Biocatalysis and Enzyme Engineering, National & Local Joint Engineering Research Center of High-throughput Drug Screening Technology, School of Life Sciences, Hubei University Wuhan 430062 China [email protected] [email protected].
  • 2. Department of Immunology and Pathogen Biology, School of Basic Medical Sciences, Hangzhou Normal University Hangzhou 311121 China.
PMID: 39823043 DOI: 10.1039/d4md00961d
Abstract

Despite the success of endocrine therapies in treating ER-positive breast Cancer, the development of resistance remains a significant challenge. Estrogen receptor targeting proteolysis-targeting chimeras (ER PROTACs) offer a unique approach by harnessing the ubiquitin-proteasome system to degrade ER, potentially bypassing resistance mechanisms. In this review, we present the drug design, efficacy and early clinical trials of these ER PROTACs. This review underscores the academic and industrial opportunities presented by this emerging technology, as well as the challenges that must be addressed to translate these findings into effective clinical therapies.

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