SERDs: a case study in targeted protein degradation

Lucia Wang, Abhishek Sharma

Research output: Contribution to journalReview articlepeer-review

5 Scopus citations

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.

Original languageEnglish
Pages (from-to)8149-8159
Number of pages11
JournalChemical Society Reviews
Volume51
Issue number19
DOIs
StatePublished - 8 Sep 2022

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