BRAF inhibitors promote intermediate BRAF(V600E) conformations and binary interactions with activated RAS.
Science Advances
Röck, Ruth R; Mayrhofer, Johanna E JE; Torres-Quesada, Omar O; Enzler, Florian F; Raffeiner, Andrea A; Raffeiner, Philipp P; Feichtner, Andreas A; Huber, Roland G RG; Koide, Shohei S; Taylor, Susan S SS; Troppmair, Jakob J; Stefan, Eduard E
Tumours with class 3 BRAF mutants are sensitive to the inhibition of activated RAS.
Nature
Yao, Zhan Z; Yaeger, Rona R; Rodrik-Outmezguine, Vanessa S VS; Tao, Anthony A; Torres, Neilawattie M NM; Chang, Matthew T MT; Drosten, Matthias M; Zhao, Huiyong H; Cecchi, Fabiola F; Hembrough, Todd T; Michels, Judith J; Baumert, Hervé H; Miles, Linde L; Campbell, Naomi M NM; de Stanchina, Elisa E; Solit, David B DB; Barbacid, Mariano M; Taylor, Barry S BS; Rosen, Neal N
Inhibitors that stabilize a closed RAF kinase domain conformation induce dimerization.
Nature Chemical Biology
Lavoie, Hugo H; Thevakumaran, Neroshan N; Gavory, Gwenaëlle G; Li, John J JJ; Padeganeh, Abbas A; Guiral, Sébastien S; Duchaine, Jean J; Mao, Daniel Y L DY; Bouvier, Michel M; Sicheri, Frank F; Therrien, Marc M