Recent advance of ATP citrate lyase inhibitors for the treatment of cancer and related diseases.
ACLY
Cancer
Inhibitors
Lipidic metabolism
SAR studies
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
Jan 2024
Jan 2024
Historique:
received:
14
07
2023
revised:
25
09
2023
accepted:
20
10
2023
medline:
28
11
2023
pubmed:
28
10
2023
entrez:
27
10
2023
Statut:
ppublish
Résumé
ATP citrate lyase (ACLY), a strategic metabolic enzyme that catalyzes the glycolytic to lipidic metabolism, has gained increasing attention as an attractive therapeutic target for hyperlipidemia, cancers and other human diseases. Despite of continual research efforts, targeting ACLY has been very challenging. In this field, most reported ACLY inhibitors are "substrate-like" analogues, which occupied with the same active pockets. Besides, some ACLY inhibitors have been disclosed through biochemical screening or high throughput virtual screening. In this review, we briefly summarized the cancer-related functions and the recent advance of ACLY inhibitors with a particular focus on the SAR studies and their modes of action. We hope to provide a timely and updated overview of ACLY and the discovery of new ACLY inhibitors.
Identifiants
pubmed: 37890210
pii: S0045-2068(23)00594-1
doi: 10.1016/j.bioorg.2023.106933
pii:
doi:
Substances chimiques
ATP Citrate (pro-S)-Lyase
EC 2.3.3.8
Types de publication
Journal Article
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
106933Informations de copyright
Copyright © 2023. Published by Elsevier Inc.
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.