Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRAS
Journal
Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531
Informations de publication
Date de publication:
12 05 2022
12 05 2022
Historique:
pubmed:
27
4
2022
medline:
18
5
2022
entrez:
26
4
2022
Statut:
ppublish
Résumé
KRAS is an archetypal high-value intractable oncology drug target. The glycine to cysteine mutation at codon 12 represents an Achilles heel that has now rendered this important GTPase druggable. Herein, we report our structure-based drug design approach that led to the identification of
Identifiants
pubmed: 35471939
doi: 10.1021/acs.jmedchem.2c00369
doi:
Substances chimiques
Antineoplastic Agents
0
KRAS protein, human
0
Quinazolines
0
Proto-Oncogene Proteins p21(ras)
EC 3.6.5.2
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM