2. Academic Validation
  3. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway

Identification of pharmacological inhibitors of the MEK5/ERK5 pathway

  • Biochem Biophys Res Commun. 2008 Dec 5;377(1):120-5. doi: 10.1016/j.bbrc.2008.09.087.
Revati J Tatake 1,  Margaret M O'Neill,  Charles A Kennedy,  Anita L Wayne,  Scott Jakes,  Di Wu,  Stanley Z Kugler Jr,  Mohammed A Kashem,  Paul Kaplita,  Roger J Snow
Affiliations

Affiliation

  • 1 Department of Cardiovascular Disease, Boehringer Ingelheim Pharmaceuticals, Inc, Ridgefield, CT 06877, USA.
PMID: 18834865 DOI: 10.1016/j.bbrc.2008.09.087
Abstract

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.

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