Crystallographic and Receptor Binding Characterization of Plasmodium falciparum Macrophage Migration Inhibitory Factor Complexed to Two Potent Inhibitors | Zendy

Georgios Pantouris | Zendy; Deepa Rajasekaran | Zendy; Alvaro Baeza Garcia | Zendy; Victor G. Ruiz | Zendy; Lin Leng | Zendy; William L. Jorgensen | Zendy; Richard Bucala | Zendy; Elias Lolis | Zendy

Open Access

Crystallographic and Receptor Binding Characterization of Plasmodium falciparum Macrophage Migration Inhibitory Factor Complexed to Two Potent Inhibitors

Author(s) -

Georgios Pantouris,

Deepa Rajasekaran,

Alvaro Baeza Garcia,

Victor G. Ruiz,

Lin Leng,

William L. Jorgensen,

Richard Bucala,

Elias Lolis

Publication year - 2014

Publication title -

journal of medicinal chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.01

H-Index - 261

eISSN - 1520-4804

pISSN - 0022-2623

DOI - 10.1021/jm501168q

Subject(s) - chemistry , plasmodium falciparum , macrophage migration inhibitory factor , inhibitory postsynaptic potential , macrophage , receptor , in vitro , biochemistry , stereochemistry , malaria , immunology , cytokine , endocrinology , biology , medicine

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.

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