Malolactone strikes: K-Ras-G12D's Achilles' heel.
Trends Pharmacol Sci
; 45(6): 472-474, 2024 Jun.
Article
em En
| MEDLINE
| ID: mdl-38653668
ABSTRACT
In a recent study in Nature Chemical Biology, Zheng et al. exploiting strain release by malolactone-based electrophiles designed a first-in-class covalent inhibitor that targets the elusive aspartate of the Kirsten rat sarcoma viral oncogene homolog (K-Ras)-G12D variant, which is highly prevalent in pancreatic cancer. The compound drastically inhibited oncogenic signaling and tumor growth in preclinical K-Ras-G12D-mutant pancreatic cancer models, expanding treatment potential beyond K-Ras-G12C-targeted therapies.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Neoplasias Pancreáticas
/
Proteínas Proto-Oncogênicas p21(ras)
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Trends Pharmacol Sci
Ano de publicação:
2024
Tipo de documento:
Article