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  3. Targeting the Estrogen Receptor for the Treatment of Breast Cancer: Recent Advances and Challenges

Targeting the Estrogen Receptor for the Treatment of Breast Cancer: Recent Advances and Challenges

  • J Med Chem. 2023 Jul 13;66(13):8339-8381. doi: 10.1021/acs.jmedchem.3c00136.
Rohan Kalyan Rej 1 2,  Junius Eugene Thomas 2nd 1 2 3,  Ranjan Kumar Acharyya 1 2,  James Michael Rae 1 2 4,  Shaomeng Wang 1 2 4 5 3
Affiliations

Affiliations

  • 1 Rogel Cancer Center, University of Michigan, Ann Arbor, Michigan 48109, United States.
  • 2 Department of Internal Medicine, University of Michigan, Ann Arbor, Michigan 48109, United States.
  • 3 Program in Chemical Biology, University of Michigan, Ann Arbor, Michigan 48109, United States.
  • 4 Department of Pharmacology, University of Michigan, Ann Arbor, Michigan 48109, United States.
  • 5 Department of Medicinal Chemistry, University of Michigan, Ann Arbor, Michigan 48109, United States.
PMID: 37377342 DOI: 10.1021/acs.jmedchem.3c00136
Abstract

Estrogen receptor alpha (ERα) is a well-established therapeutic target for the treatment of ER-positive (ER+) breast cancers. Despite the tremendous successes achieved with tamoxifen, a selective ER modulator, and aromatase inhibitors (AIs), resistance to these therapies is a major clinical problem. Therefore, induced protein degradation and covalent inhibition have been pursued as new therapeutic approaches to target ERα. This Perspective summarizes recent progress in the discovery and development of oral selective ER degraders (SERDs), complete Estrogen receptor antagonists (CERANs), selective Estrogen receptor covalent antagonists (SERCAs), and proteolysis targeting chimera (PROTAC) ER degraders. We focus on those compounds which have been advanced into clinical development.

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