Inhibitors bind and inhibit highly active BRAF mutants

Stable Identifier
Reaction [binding]
Homo sapiens
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The class I ATP competitive inhibitors vemurafenib and dabrafenib have been approved for treatment of V600E melanoma, and other BRAF-selective inhibitors are in clinical and preclinical trials. These inhibitors bind to the active conformation of the enzyme promoted by the V600E mutation (King et al, 2006; Tsai et al, 2008).

Literature References
PubMed ID Title Journal Year
18287029 Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity

Tsai, J, Lee, JT, Wang, W, Zhang, J, Cho, H, Mamo, S, Bremer, R, Gillette, S, Kong, J, Haass, NK, Sproesser, K, Li, L, Smalley, KS, Fong, D, Zhu, YL, Marimuthu, A, Nguyen, H, Lam, B, Liu, J, Cheung, I, Rice, J, Suzuki, Y, Luu, C, Settachatgul, C, Shellooe, R, Cantwell, J, Kim, SH, Schlessinger, J, Zhang, KY, West, BL, Powell, B, Habets, G, Zhang, C, Ibrahim, PN, Hirth, P, Artis, DR, Herlyn, M, Bollag, G

Proc. Natl. Acad. Sci. U.S.A. 2008
17145850 Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885

King, AJ, Patrick, DR, Batorsky, RS, Ho, ML, Do, HT, Zhang, SY, Kumar, R, Rusnak, DW, Takle, AK, Wilson, DM, Hugger, E, Wang, L, Karreth, F, Lougheed, JC, Lee, J, Chau, D, Stout, TJ, May, EW, Rominger, CM, Schaber, MD, Luo, L, Lakdawala, AS, Adams, JL, Contractor, RG, Smalley, KS, Herlyn, M, Morrissey, MM, Tuveson, DA, Huang, PS

Cancer Res. 2006
Participant Of
Name Identifier Synonyms
cancer 162 malignant tumor, malignant neoplasm, primary cancer
cardiofaciocutaneous syndrome 0060233 CFC syndrome, cardio-facial-cutaneous syndrome
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