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Selective and noncovalent targeting of RAS mutants for inhibition and degradation

Nat Commun. 2021-05; 
Kai Wen Teng, Steven T Tsai, Takamitsu Hattori, Carmine Fedele, Akiko Koide, Chao Yang, Xuben Hou, Yingkai Zhang, Benjamin G Neel, John P O'Bryan, Shohei Koide
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Catalog Antibody … The relative concentrations of intracellular FLAG-tagged monobody inhibitor or HA-tagged monobodies were determined by comparing the intensity of protein bands with the intensity of the bands from equal amounts of loading control proteins (GenScript, M0101) containing … Get A Quote

摘要

Activating mutants of RAS are commonly found in human cancers, but to date selective targeting of RAS in the clinic has been limited to KRAS(G12C) through covalent inhibitors. Here, we report a monobody, termed 12VC1, that recognizes the active state of both KRAS(G12V) and KRAS(G12C) up to 400-times more tightly than wild-type KRAS. The crystal structures reveal that 12VC1 recognizes the mutations through a shallow pocket, and 12VC1 competes against RAS-effector interaction. When expressed intracellularly, 12VC1 potently inhibits ERK activation and the proliferation of RAS-driven cancer cell lines in vitro and in mouse xenograft models. 12VC1 fused to VHL selectively degrades the KRAS mutants and provides more ... More

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