Recent Advances of MEK Inhibitors and Their Clinical Progress

Authors: John Yuan, Wang¹; Keith, Wilcoxen M.¹; Kenichi, Nomoto¹; Sara, Wu¹

Source: Current Topics in Medicinal Chemistry, Volume 7, Number 14, July 2007 , pp. 1364-1378(15)

Publisher: Bentham Science Publishers

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Abstract:

The RAS/RAF/MEK/ERK signaling pathway has been a major clinical focus in oncology research in recent years. A clearer association of B-RAF mutations to cancers such as melanoma, papillary thyroid cancer and others has brought an increasing interest in chemotherapeutics that target this cellular signaling pathway. In this review, the authors summarize the current understanding of science and therapeutic use of the MEK inhibitors targeting the RAS/RAF/ MEK/ERK pathway. Clinical progresses of PD0325901 and AZD6244 are highlighted in addition to developments of new MEK inhibitors. Recently disclosed MEK inhibitors in two sub-divided classes, ATP noncompetitive and ATP competitive inhibitors are discussed.

Keywords: MEK inhibitors; RAF kinase; B-RAF mutation; MEK kinase; PD0325901; AZD6244; hypothemycin; resorcylic acid lactones

Document Type: Research article

DOI: 10.2174/156802607781696837

Affiliations: 1: Eisai Research Institute of Boston Inc., 4 Corporate Drive, Andover, MA 01810, USA.

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