SERDs: a case study in targeted protein degradation. (8th September 2022)

• Record Type: Journal Article
• Authors: Wang, Lucia; Sharma, Abhishek
• Is Part Of: Chemical Society reviews. Volume 51:Number 19(2022)
• Page Start: 8149
• Page End: 8159
• Publication Date: 2022-09-08
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1039/d2cs00117a
• Languages: English
• ISSNs: 0306-0012

Abstract

Abstract : This tutorial review summarizes the recent progress of SERDs and their mechanism of action in the broader context of 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.