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Curr Opin Investig Drugs. 2007 Jun;8(6):452-6.

B-Raf kinase inhibitors for cancer treatment.

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Genomics Institute of the Novartis Research Foundation, Kinase Platform, 10675 John Jay Hopkins Drive, San Diego, CA 92121, USA.


The Raf-MEK-ERK signaling pathway is critical for cell survival, growth, proliferation and tumorigenesis. Among the three isoforms of Raf protein kinases, in vitro and in vivo studies have shown that B-Raf functions as the primary MEK activator. B-Raf is one of the most frequently mutated genes in human cancers with a high prevalence in melanoma, and many of the B-Raf mutations activate the kinase activity of B-Raf. B-Raf kinase represents an excellent target for anticancer therapy based on preclinical target validation, epidemiology and drugability. Several small-molecule inhibitors of B-Raf kinase are currently undergoing clinical evaluation, with others due to enter clinical development in the near future.

[Indexed for MEDLINE]

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