NYMC Faculty Publications

B-Raf and the Inhibitors: From Bench to Bedside

Author Type(s)

Faculty

DOI

10.1186/1756-8722-6-30

Journal Title

Journal of Hematology & Oncology

First Page

30

Last Page

30

Document Type

Article

Publication Date

4-25-2013

Department

Pathology, Microbiology and Immunology

Keywords

Animals, Cell Line, Tumor, Humans, MAP Kinase Signaling System, Neoplasms, Protein Kinase Inhibitors, Proto-Oncogene Proteins B-raf

Disciplines

Medicine and Health Sciences | Oncology | Pathology

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.

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