Issue 19, 2022

SERDs: a case study in targeted protein degradation

Abstract

Endocrine therapies for breast cancer target ERα which is found in more than 70% of breast cancers. Unfortunately, endocrine resistance typically occurs, in which case Selective Estrogen Receptor Degraders (SERDs) represent the last line of treatment for metastatic breast cancer patients. Fulvestrant, the only currently approved SERD and one of the first targeted protein degradation therapies, presents poor drug-like properties which has led to the development of a new generation of oral SERDs. This review summarizes recent progress in the evolution of SERDs, focusing on clinical candidates and their degradation motifs within the broader context of targeted protein degradation therapies.

Graphical abstract: SERDs: a case study in targeted protein degradation

Article information

Article type
Tutorial Review
Submitted
09 Feb 2022
First published
08 Sep 2022

Chem. Soc. Rev., 2022,51, 8149-8159

Author version available

SERDs: a case study in targeted protein degradation

L. Wang and A. Sharma, Chem. Soc. Rev., 2022, 51, 8149 DOI: 10.1039/D2CS00117A

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