B-Raf and the inhibitors: from bench to bedside

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 evaluat...

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Autores principales: Huang, Tiangui, Karsy, Michael, Zhuge, Jian, Zhong, Minghao, Liu, Delong
Formato: Online Artículo Texto
Lenguaje:English
Publicado: BioMed Central 2013
Materias:
Review
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3646677/
https://www.ncbi.nlm.nih.gov/pubmed/23617957
http://dx.doi.org/10.1186/1756-8722-6-30
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author Huang, Tiangui
Karsy, Michael
Zhuge, Jian
Zhong, Minghao
Liu, Delong
author_facet Huang, Tiangui
Karsy, Michael
Zhuge, Jian
Zhong, Minghao
Liu, Delong
author_sort Huang, Tiangui
collection PubMed
description 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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spelling pubmed-36466772013-05-08 B-Raf and the inhibitors: from bench to bedside Huang, Tiangui Karsy, Michael Zhuge, Jian Zhong, Minghao Liu, Delong J Hematol Oncol Review 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. BioMed Central 2013-04-25 /pmc/articles/PMC3646677/ /pubmed/23617957 http://dx.doi.org/10.1186/1756-8722-6-30 Text en Copyright © 2013 Huang et al.; licensee BioMed Central Ltd. http://creativecommons.org/licenses/by/2.0 This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Review
Huang, Tiangui
Karsy, Michael
Zhuge, Jian
Zhong, Minghao
Liu, Delong
B-Raf and the inhibitors: from bench to bedside
title B-Raf and the inhibitors: from bench to bedside
title_full B-Raf and the inhibitors: from bench to bedside
title_fullStr B-Raf and the inhibitors: from bench to bedside
title_full_unstemmed B-Raf and the inhibitors: from bench to bedside
title_short B-Raf and the inhibitors: from bench to bedside
title_sort b-raf and the inhibitors: from bench to bedside
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3646677/
https://www.ncbi.nlm.nih.gov/pubmed/23617957
http://dx.doi.org/10.1186/1756-8722-6-30
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