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Article

Protomer selectivity of type II RAF inhibitors within the RAS/RAF complex.

Cell chemical biology - 16 Nov 2023

Vasta James D, Michaud Ani, Zimprich Chad A, Beck Michael T, Swiatnicki Matthew R, Zegzouti Hicham, Thomas Morgan R, Wilkinson Jennifer, Crapster J Aaron, Robers Matthew B

Abstract excerpt

RAF dimer inhibitors offer therapeutic potential in RAF- and RAS-driven cancers. The utility of such drugs is predicated on their capacity to occupy both RAF protomers in the RAS-RAF signaling complex. Here we describe a method to conditionally quantify drug-target occupancy at selected RAF protomers within an active RAS-RAF complex in cells. RAF target engagement can be measured in the presence or absence of any...

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Methodology Data sources Editorial policy Privacy Delete account & data About Contact Helena Bioinformatics

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Identifiers

PMID: 37643616
DOI: 10.1016/j.chembiol.2023.07.019

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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