Design and Synthesis of Type-IV Inhibitors of BRAF Kinase That Block Dimerization and Overcome Paradoxical MEK/ERK Activation.
Journal Of Medicinal Chemistry
Beneker, Chad M CM; Rovoli, Magdalini M; Kontopidis, George G; Röring, Michael M; Galda, Simeon S; Braun, Sandra S; Brummer, Tilman T; McInnes, Campbell C
N-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl)phenyl)acetamido)phenoxy)benzo[d]thiazol-2-yl)cyclopropanecarboxamide (TAK632) Promotes Inhibition of BRAF through the Induction of Inhibited Dimers.
Journal Of Medicinal Chemistry
Grasso, Michael M; Estrada, Michelle A MA; Berrios, Kiara N KN; Winkler, Jeffrey D JD; Marmorstein, Ronen R
Distinct requirement for an intact dimer interface in wild-type, V600E and kinase-dead B-Raf signalling.
The Embo Journal
Röring, Michael M; Herr, Ricarda R; Fiala, Gina J GJ; Heilmann, Katharina K; Braun, Sandra S; Eisenhardt, Anja E AE; Halbach, Sebastian S; Capper, David D; von Deimling, Andreas A; Schamel, Wolfgang W WW; Saunders, Darren N DN; Brummer, Tilman T