TY - JOUR
T1 - SERDs
T2 - a case study in targeted protein degradation
AU - Wang, Lucia
AU - Sharma, Abhishek
N1 - Publisher Copyright:
© 2022 The Royal Society of Chemistry.
PY - 2022/9/8
Y1 - 2022/9/8
N2 - 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.
AB - 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.
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U2 - 10.1039/d2cs00117a
DO - 10.1039/d2cs00117a
M3 - Review article
C2 - 36073297
AN - SCOPUS:85138669764
SN - 0306-0012
VL - 51
SP - 8149
EP - 8159
JO - Chemical Society Reviews
JF - Chemical Society Reviews
IS - 19
ER -