Inhibition of Son of Sevenless Homologue 1 (SOS1): Promising therapeutic treatment for KRAS-mutant cancers.
Cancer therapy
KRAS
PROTACs
SOS1 inhibitors
Small molecules
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 Dec 2023
05 Dec 2023
Historique:
received:
04
07
2023
revised:
19
09
2023
accepted:
21
09
2023
medline:
3
11
2023
pubmed:
2
10
2023
entrez:
1
10
2023
Statut:
ppublish
Résumé
Kristen rat sarcoma (KRAS) is one of the most common oncogenes in human cancers. As a guanine nucleotide exchange factor, Son of Sevenless Homologue 1 (SOS1) represents a potential therapeutic concept for the treatment of KRAS-mutant cancers because of its activation on KRAS and downstream signaling pathways. In this review, we provide a comprehensive overview of the structure, biological function, and regulation of SOS1. We also focus on the recent advances in SOS1 inhibitors and emphasize their binding modes, structure-activity relationships and pharmacological activities. We hope that this publication can provide a comprehensive compendium on the rational design of SOS1 inhibitors.
Identifiants
pubmed: 37778239
pii: S0223-5234(23)00795-X
doi: 10.1016/j.ejmech.2023.115828
pii:
doi:
Substances chimiques
Proto-Oncogene Proteins p21(ras)
EC 3.6.5.2
SOS1 Protein
0
KRAS protein, human
0
Types de publication
Journal Article
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
115828Informations 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.