Inhibitors bind and inhibit highly active BRAF mutants

Stable Identifier
Reaction [binding]
Homo sapiens
Locations in the PathwayBrowser
SVG |   | PPTX  | SBGN
Click the image above or here to open this reaction in the Pathway Browser
The layout of this reaction may differ from that in the pathway view due to the constraints in pathway layout

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
17145850 Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885

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

Cancer Res. 2006
18287029 Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity

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

Proc. Natl. Acad. Sci. U.S.A. 2008
Functional status
Name Identifier Synonyms
cardiofaciocutaneous syndrome DOID:0060233 CFC syndrome, cardio-facial-cutaneous syndrome
cancer DOID:162 malignant tumor, malignant neoplasm, primary cancer
Cite Us!