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J Med Chem. 2014 Oct 23;57(20):8652-6. doi: 10.1021/jm501168q. Epub 2014 Oct 8.

Crystallographic and receptor binding characterization of Plasmodium falciparum macrophage migration inhibitory factor complexed to two potent inhibitors.

Author information

1
Departments of Pharmacology, ‡Internal Medicine, §Chemistry, and the ∥Yale Cancer Center, Yale University , New Haven, Connecticut 06520-8066, United States.

Abstract

We report the crystal structures of two inhibitors of Plasmodium falciparum macrophage migration inhibitory factor (PfMIF) with nanomolar Ki's, analyze their interactions with the active site of PfMIF, and provide explanations regarding their selectivity of PfMIF versus human MIF. These inhibitors were also found to selectively inhibit interactions between PfMIF and the human MIF receptor CD74. The results of this study provide the framework for the development of new therapeutics that target PfMIF.

PMID:
25268646
PMCID:
PMC4207548
DOI:
10.1021/jm501168q
[Indexed for MEDLINE]
Free PMC Article

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