RAF inhibitor PLX8394 selectively disrupts BRAF dimers and RAS-independent BRAF-mutant-driven signaling.
Yao Z, Gao Y, Su W, Yaeger R, Tao J, Na N, Zhang Y, Zhang C, Rymar A, Tao A, Timaul NM, Mcgriskin R, Outmezguine NA, Zhao H, Chang Q, Qeriqi B, Barbacid M, de Stanchina E, Hyman DM, Bollag G, Rosen N.
Yao Z, et al.
Nat Med. 2019 Feb;25(2):284-291. doi: 10.1038/s41591-018-0274-5. Epub 2018 Dec 17.
Nat Med. 2019.
PMID: 30559419
Free PMC article.
We show here that PLX8394, a new RAF inhibitor(9), inhibits ERK signaling by specifically disrupting BRAF-containing dimers, including BRAF homodimers and BRAF-CRAF heterodimers, but not CRAF homodimers or ARAF-containing dimers. Differences in the amino acid residu …
We show here that PLX8394, a new RAF inhibitor(9), inhibits ERK signaling by specifically disrupting BRAF-containing dimers, including BRAF …