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
Current Topics in Medicinal Chemistry
Title: Recent Advances of MEK Inhibitors and Their Clinical Progress
Volume: 7 Issue: 14
Author(s): Wang John (Yuan), Wilcoxen M. Keith, Nomoto Kenichi and Wu Sara
Affiliation:
Keywords: MEK inhibitors, RAF kinase, B-RAF mutation, MEK kinase, PD0325901, AZD6244, hypothemycin, resorcylic acid lactones
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.
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John (Yuan) Wang, Keith M. Wilcoxen, Kenichi Nomoto and Sara Wu, Recent Advances of MEK Inhibitors and Their Clinical Progress, Current Topics in Medicinal Chemistry 2007; 7 (14) . https://dx.doi.org/10.2174/156802607781696837
DOI https://dx.doi.org/10.2174/156802607781696837 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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