Article
Malolactone strikes: K-Ras-G12D's Achilles' heel.
Trends in pharmacological sciences - 1 Jun 2024
Adamopoulos Christos, Papavassiliou Kostas A, Papavassiliou Athanasios G
Abstract excerpt
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...
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