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Assessment of KRAS G12C Target Engagement by a Covalent Inhibitor in Tumor Biopsies Using an Ultra-Sensitive Immunoaffinity 2D-LC-MS/MS Approach.

Analytical chemistry - 20 Sept 2022

Meng Lingyao, Chan Emily W, Ng Carl, Aimi Junko, Tran John C, Oh Angela J, Merchant Mark, Purkey Hans E, Heffron Timothy P, Kaur Surinder, Xu Keyang, Shi Zhen, He Jintang

Abstract excerpt

KRAS is one of the most frequently mutated oncogenes, with KRAS G12C recently becoming an actionable target for small molecule intervention. GDC-6036 is an investigational KRAS G12C inhibitor that acts by irreversibly binding to the switch II pocket of KRAS G12C when in the inactive GDP-bound state, thereby blocking GTP binding and activation. Assessing target engagement is an essential component of clinical drug...

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PMID: 36083155
DOI: 10.1021/acs.analchem.2c03146

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