Characterization and inhibitor sensitivity of ARAF, BRAF, and CRAF kinases.

ABSTRACT: The RAS-RAF-MEK-ERK signaling pathway controls cellular growth and proliferation, and mutational activation of this pathway is a frequent cause of cancer. Most prominently, the V600E mutation in BRAF causes malignant melanoma, papillary thyroid cancer, and other malignancies. Rare but recurrent activating mutations in the other two RAF isoforms, ARAF and CRAF, have also been identified in diverse cancers. Distinct classes of RAF inhibitors have been developed, particularly for BRAF^V600E, but their potencies against the three RAF isoforms have not been systematically compared. Here, we biochemically characterize monomeric and dimeric preparations of ARAF, BRAF, and CRAF kinases and measure the potencies of a panel of thirteen type I, type I.5, and type II RAF inhibitors against e

SUBMITTER: Tkacik E 

PROVIDER: S-EPMC12630025 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature