Fig. 1: BRAF mutation classes and mechanism of actions for BRAF/MEK inhibitors.
From: BRAFV600E-mutant metastatic NSCLC: disease overview and treatment landscape
Class I and II mutations are RAS-independent, constitutively active monomers (class I) or dimers (class II). Class III mutations are RAS-dependent dimers with compromised kinase activity. Current BRAF inhibitors are effective for class I-mutant monomers. Next-generation RAF inhibitors can inhibit dimers and may inhibit class II and III mutations. P, phosphorylation.
