Identification of benzimidazole-based inhibitors of the mitogen activated kinase-5 signaling pathway.
The MEK-signaling pathways are complex but critical signaling cascades that correlate an extracellular signaling event with internal cell processes. To date at least seven MEK isozymes have been identified. MEK5, in particular, is upregulated in multiple forms of tumors. Analysis of the EGF-induced MEK5 signaling cascade in cultured HEK cells has identified compounds that can inhibit MEK5 phosphorylation of ERK5; observed biological activity is dependent on chemical variation.
Flaherty
Patrick T
PT
Division of Medicinal Chemistry, School of Pharmacy, Duquesne University, 600 Forbes Ave., Pittsburgh, PA 15282, USA. flahertyp@duq.edu
Chopra
Ishveen
I
Jain
Prashi
P
Yi
Shuyan
S
Allen
Erika
E
Cavanaugh
Jane
J
D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D004815:Epidermal Growth Factor / Q000494:pharmacology; D006801:Humans; D048671:MAP Kinase Kinase 5 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D048054:Mitogen-Activated Protein Kinase 7 / Q000378:metabolism; D010766:Phosphorylation; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D015398:Signal Transduction / Q000187:drug effects*
D001562:Benzimidazoles; D047428:Protein Kinase Inhibitors; D004815:Epidermal Growth Factor; D048054:Mitogen-Activated Protein Kinase 7; D048671:MAP Kinase Kinase 5