Work

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

Year: 2023

Type: article

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.

Source: Journal of Medicinal Chemistry

DOI: 10.1021/acs.jmedchem.3c00136

Authors: Rohan Kalyan Rej, Junius Eugene Thomas, Ranjan Kumar Acharyya, James Michael Rae, Shaomeng Wang

Institutions: University of Michigan, U-M Rogel Cancer Center

Language: English

Topic: Estrogen and related hormone effects

Subfield: Genetics

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: green

Funder: National Institutes of Health