Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 23, Pages 7033-7036Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.09.118
Keywords
MIF; Cytokine; Agonists; Structure-based design; AMPK activation; ERK phosphorylation; Click chemistry
Categories
Funding
- National Institutes of Health [AI042310, AR049610, AR050498, GM032136]
- Treat B. Johnson Fund at Yale
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The cytokine MIF is involved in inflammation and cell proliferation via pathways initiated by its binding to the transmembrane receptor CD74. MIF also promotes AMPK activation with potential benefits for response to myocardial infarction and ischemia-reperfusion. Structure-based molecular design has led to the discovery of not only antagonists, but also the first agonists of MIF-CD74 binding. The compounds contain a triazole core that is readily assembled via Cu-catalyzed click chemistry. The agonist and antagonist behaviors were confirmed via study of MIF-dependent ERK1/2 phosphorylation in human fibroblasts. (C) 2010 Elsevier Ltd. All rights reserved.
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