B-Raf and the inhibitors: from bench to bedside

  • J Hematol Oncol. 2013 Apr 25:6:30. doi: 10.1186/1756-8722-6-30.
Tiangui Huang  1 ,  Michael Karsy ,  Jian Zhuge ,  Minghao Zhong ,  Delong Liu
Affiliations
  • 1. Department of Pathology, Westchester Medical Center and New York Medical College, Valhalla, NY 10595, USA.
PMID: 23617957 DOI: 10.1186/1756-8722-6-30
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.

Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-16063
    ARQ-736
    B-RAF Inhibitor
    target: Raf
    Research Areas: Cancer