Selective Estrogen receptor degraders (SERDs) for the treatment of breast cancer: An overview.
Anti-estrogenic
Aromatase
Breast cancer
ER-α
ER-β
Elacestrant
Estrogen
Fulvestrant
Orserdu
SERM
Selective estrogen receptor degraders (SERDs)
Journal
European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510
Informations de publication
Date de publication:
05 Aug 2023
05 Aug 2023
Historique:
received:
14
03
2023
revised:
17
04
2023
accepted:
26
04
2023
medline:
2
6
2023
pubmed:
11
5
2023
entrez:
10
5
2023
Statut:
ppublish
Résumé
Discovery of SERDs has changed the direction of anticancer research, as more than 70% of breast cancer cases are estrogen receptor positive (ER+). Therapies such as selective estrogen receptor modulators (SERM) and aromatase inhibitors (AI's) have been effective, but due to endocrine resistance, SERDs are now considered essential therapeutics for the treatment of ER+ breast cancer. The present review deliberates the pathophysiology of SERDs from the literature covering various molecules in clinical trials. Estrogen receptors active sites distinguishing characteristics and interactions with currently available FDA-approved drugs have also been discussed. Designing strategy of previously reported SERDs, their SAR analysis, in silico, and the biological efficacy have also been summarized along with appropriate examples.
Identifiants
pubmed: 37163948
pii: S0223-5234(23)00388-4
doi: 10.1016/j.ejmech.2023.115422
pii:
doi:
Substances chimiques
Receptors, Estrogen
0
Estrogen Antagonists
0
Selective Estrogen Receptor Modulators
0
Aromatase Inhibitors
0
Estrogen Receptor alpha
0
Types de publication
Journal Article
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
115422Informations de copyright
Copyright © 2023 Elsevier Masson SAS. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.