Author

Anne Y. Saiki

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Open access Jul 2026

Property-Biased Covalent DNA-Encoded Library Screening Enabled the Discovery of AM-8719, A Structurally Novel, CNS-Penetrant KRAS G12C Inhibitor

Activating mutations in the Kirsten rat sarcoma (KRAS) gene are prevalent oncogenic drivers in nonsmall cell lung cancer (NSCLC). Patients harboring KRAS-mutant lung cancers frequently develop central nervous system (CNS) metastases. Although approved KRAS G12C inhibitors (i.e., sotorasib and adagrasib) show promising...

Slavko Rast, Marie Morgan-Fisher, Sarah D. Blomquist et al. · Journal of Medicinal Chemist... · 1 citation

Open access Jul 2026

Expanding Addressable KRAS Mutations through the Structure- and Property-Based Design of Dual-State (GDP/GTP), Reversible Pan-KRAS Inhibitors

AM-2383 represents an important proof-of-concept that structural insights from prior covalent KRASG12C inhibitors can be leveraged in the design of efficacious and well-tolerated inhibitors of diverse KRAS mutations.

Ryan P. Wurz, Jennifer R. Allen, J. Allen et al. · Journal of Medicinal Chemist... · 0 citations