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Current Topics in Medicinal Chemistry


ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Progress Towards Therapeutic Small Molecule MEK Inhibitors for Use in Cancer Therapy

Author(s): Eli M. Wallace, Joseph P. Lyssikatos, Tammie Yeh, James D. Winkler and Kevin Koch

Volume 5, Issue 2, 2005

Page: [215 - 229] Pages: 15

DOI: 10.2174/1568026053507723

Price: $65


This paper reviews recent progress in the design and evaluation of MEK inhibitors as cancer therapeutics. Activation of the Ras / Raf / MEK / MAP kinase pathway has been implicated in uncontrolled cell proliferation and tumor growth. Mutated, oncogenic forms of Ras are found in 50% of colon, 90% of pancreatic and 30% of lung cancers. Recently, B-Raf mutations have been identified in more than 60% of malignant melanomas and from 40-70% of papillary thyroid cancers. MEK, a dual specificity kinase, is a key player in this pathway; it is downstream of both Ras and Raf and activates ERK1/2 through phosphorylation of key tyrosine and threonine residues. Representative examples of both ATP competitive and non-competitive inhibitors as well as natural product based inhibitors will be discussed.

Keywords: mek inhibitor, erk, arry-142886 (azd 6244), pd 0325901, ci-1040, cancer, map kinase, kinase inhibitor

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