Aromatase inhibitors for the treatment of breast cancer: An overview (2019-2023).
Aromatase
Aromatase inhibitors
Breast cancer
ER-positive
Estrogen
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
04 Jul 2024
04 Jul 2024
Historique:
received:
18
04
2024
revised:
02
06
2024
accepted:
28
06
2024
medline:
14
7
2024
pubmed:
14
7
2024
entrez:
13
7
2024
Statut:
aheadofprint
Résumé
Aromatase inhibition is considered a legitimate approach for the treatment of ER-positive (ER+) breast cancer as it accounts for more than 70% of breast cancer cases. Aromatase inhibitor therapy has been demonstrated to be highly effective in decreasing tumour size, increasing survival rates, and lowering the chance of cancer recurrence. The present review deliberates the pathophysiology and the role of aromatase in estrogen biosynthesis. Estrogen biosynthesis, various androgens, and their function in the human body have also been discussed. The salient aspects of the aromatase active site, its mode of action, and AIs, along with their intended interactions with presently FDA-approved inhibitors, have been briefly discussed. It has been detailed how different reported AIs were designed, their SAR investigations, in silico analysis, and biological evaluations. Various AIs from multiple origins, such as synthetic and semi-synthetic, have also been discussed.
Identifiants
pubmed: 39002515
pii: S0045-2068(24)00512-1
doi: 10.1016/j.bioorg.2024.107607
pii:
doi:
Types de publication
Journal Article
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
107607Informations de copyright
Copyright © 2024 Elsevier Inc. 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.