High-resolution measurement of ERK activation state reveals determinants of BRAF regulation and drug sensitivity. (PubMed, bioRxiv) - Oct 11, 2026 - "We identified a large class of dominant negative variants that suppress signaling below endogenous levels through enhanced RAS engagement and an inability to form productive RAF dimers. Measuring the intracellular potency of the RAF inhibitor LXH254 against ∼1,000 variants in parallel revealed hinge and activation-loop positions conferring resistance and showed that disrupting the BRAF-MEK interface is broadly sensitizing."
Journal • Oncology • BRAF
|
|
A Felicia Adebanjo; Douglas M Fowler; Dustin J Maly; Fernando Banales-Mejia; Jessica J Simon
|