TITLE

B-Raf and the inhibitors: from bench to bedside

AUTHOR(S)
Tiangui Huang; Karsy, Michael; Jian Zhuge; Minghao Zhong; Delong Liu
PUB. DATE
June 2013
SOURCE
Journal of Hematology & Oncology;2013, Vol. 6 Issue 1, p1
SOURCE TYPE
Academic Journal
DOC. TYPE
Article
ABSTRACT
The B-Raf protein is a key signaling molecule in the mitogen activated protein kinase (MAPK) signaling pathway and has been implicated in the pathogenesis of a variety of cancers. An important V600E mutation has been identified and can cause constitutive B-Raf activation. Recent studies have evaluated a variety of small molecule inhibitors targeting B-Raf, including PLX4032/vemurafenib, dabrafenib, LGX818, GDC0879, XL281, ARQ736, PLX3603 (RO5212054), and RAF265. Therapeutic resistance has been identified and various mechanisms described. This review also discussed the current understanding of B-Raf signaling mechanism, methods of mutation detection, treatment strategies as well as potential methods of overcoming therapeutic resistance.
ACCESSION #
87990962

 

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