Design and Discovery of MRTX0902, a Potent, Selective, Brain-Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein-Protein Interaction.
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:
28 07 2022
28 07 2022
Historique:
pubmed:
15
7
2022
medline:
30
7
2022
entrez:
14
7
2022
Statut:
ppublish
Résumé
SOS1 is one of the major guanine nucleotide exchange factors that regulates the ability of KRAS to cycle through its "on" and "off" states. Disrupting the SOS1:KRAS
Identifiants
pubmed: 35833726
doi: 10.1021/acs.jmedchem.2c00741
pmc: PMC9340770
doi:
Substances chimiques
Acetonitriles
0
KRAS protein, human
0
Piperazines
0
Pyrimidines
0
SOS1 Protein
0
adagrasib
8EOO6HQF8Y
Proto-Oncogene Proteins p21(ras)
EC 3.6.5.2
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Research Support, U.S. Gov't, Non-P.H.S.
Langues
eng
Sous-ensembles de citation
IM
Pagination
9678-9690Subventions
Organisme : NIGMS NIH HHS
ID : P30 GM124165
Pays : United States
Organisme : NIH HHS
ID : S10 OD021527
Pays : United States
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