Despite well-established tumorigenic roles of KRAS mutants, targeting their smooth surfaces was a challenge, which was overcome through the development of G12C-specific covalent inhibitors. A new study shows that optimizing non-covalent interactions with a cryptic pocket produces remarkable potency for another hotspot mutation.

中文翻译：

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击中热点

尽管 KRAS 突变体具有公认的致瘤作用，但靶向其光滑表面是一项挑战，通过开发 G12C 特异性共价抑制剂克服了这一挑战。一项新的研究表明，优化与隐秘口袋的非共价相互作用可为另一个热点突变产生显着的效力。