期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 18, 期 22, 页码 8054-8060出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.09.017
关键词
MEK; MEK5; ERK; ERK5; Benzimidazole; Hoechst 33258
资金
- NIH (NINDS) [1R15NS057772]
- NSF [CHE-0354052, CHE 0614785]
- Duquesne University
In a prior communication we identified a novel class of benzimidazole-based inhibitors of EGF-induced phosphorylation of ERK5. In this paper we examine the biological activity of several 1-isopropyl-4-amino-6-ether linked benzimidazole-based compounds for their ability to selectively inhibit EGF-mediated ERK5 phosphorylation; potential utility of variation at the 6-position was indicated by the initial structural feature survey. Modification of EGF-induced formation of pERK1/2 and pERK5 in HEK293 cells were analyzed by Western blot analysis. Subsequent analysis of selected compounds in a high-throughput multiple kinase scan and the NCI 60-cell-line screen is presented. (C) 2010 Elsevier Ltd. All rights reserved.
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