Identification of pharmacological inhibitors of the MEK5/ERK5 pathway

被引：132

作者：

Tatake, Revati J. ^{[1
]}

O'Neill, Margaret M. ^{[1
]}

Kennedy, Charles A. ^{[1
]}

Wayne, Anita L. ^{[1
]}

Jakes, Scott ^{[1
]}

Wu, Di ^{[2
]}

Kugler, Stanley Z., Jr. ^{[2
]}

Kashem, Mohammed A. ^{[2
]}

Kaplita, Paul ^{[3
]}

Snow, Roger J. ^{[2
]}

机构：

[1] Boehringer Ingelheim Pharmaceut Inc, Dept Cardiovasc Dis, Ridgefield, CT 06877 USA

[2] Boehringer Ingelheim Pharmaceut Inc, Dept Med Chem, Ridgefield, CT 06877 USA

[3] Boehringer Ingelheim Pharmaceut Inc, Dept Drug Discovery Support, Ridgefield, CT 06877 USA

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 2008年 / 377卷 / 01期

关键词：

MEK5; ERK5; Kinase inhibitors; Pharmacological inhibitors;

D O I：

10.1016/j.bbrc.2008.09.087

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

We have identified two novel MEK5 inhibitors, BIX02188 and BIX02189, which inhibited catalytic function of purified, MEK5 enzyme. The MEK5 inhibitors blocked phosphorylation of ERK5, without affecting phosphorylation of ERK1/2 in sorbitol-stimulated HeLa cells. The compounds also inhibited transcriptional activation of MEF2C, a downstream substrate of the MEK5/ERK5 signaling cascade, in a cellular trans-reporter assay system. These inhibitors offer novel pharmacological tools to better characterize the role of the MEK5/ERK5 pathway in various biological systems. (C) 2008 Elsevier Inc. All rights reserved.

引用

页码：120 / 125

页数：6

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