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Bioorg Med Chem Lett. 2010 Dec 1;20(23):7033-6. doi: 10.1016/j.bmcl.2010.09.118. Epub 2010 Sep 29.

Receptor agonists of macrophage migration inhibitory factor.

Author information

1
Department of Chemistry, Yale University, New Haven, CT 06520, USA. william.jorgensen@yale.edu

Abstract

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.

PMID:
20971005
PMCID:
PMC2989669
DOI:
10.1016/j.bmcl.2010.09.118
[Indexed for MEDLINE]
Free PMC Article

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