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Recent Advances in the Research and Development of RAF Kinase Inhibitors

作者:Roger A. Smith, Jacques Dumas, Lila Adnane, Scott M. Wilhelm · 发表于:Current Topics in Medicinal Chemistry · 年份:2006 · DOI:10.2174/156802606777812077 · 被引用次数:48 · 研究领域:Melanoma and MAPK Pathways、Computational Drug Discovery Methods、Cancer Mechanisms and Therapy

The RAS-RAF-MEK-ERK signaling pathway (ERK pathway) plays a key role in tumorigenesis and cancer progression. Mutations of RAS or B-RAF lead to a constitutive activation of the ERK pathway, which ultimately results in increased cell division, and cell survival. This review article focuses on the recent literature related to ERK pathway inhibitors, with a particular emphasis on RAF kinase inhibitors. Preclinical and clinical data for the RAF kinase inhibitor sorafenib (BAY 43-9006 tosylate), that was recently approved in the US for the treatment of advanced renal cell carcinoma, are also outlined.