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Review
. 2018 Nov;23(11):1910-1918.
doi: 10.1016/j.drudis.2018.06.017. Epub 2018 Jun 21.

Small-molecule inhibitors of macrophage migration inhibitory factor (MIF) as an emerging class of therapeutics for immune disorders

Tjie Kok  1 , Anna A Wasiel  2 , Robbert H Cool  2 , Barbro N Melgert  3 , Gerrit J Poelarends  2 , Frank J Dekker  4
Affiliations
Review

Small-molecule inhibitors of macrophage migration inhibitory factor (MIF) as an emerging class of therapeutics for immune disorders

Tjie Kok et al. Drug Discov Today. 2018 Nov.

Abstract

Macrophage migration inhibitory factor (MIF) is an important cytokine for which an increasing number of functions is being described in the pathogenesis of inflammation and cancer. Nevertheless, the availability of potent and druglike MIF inhibitors that are well-characterized in relevant disease models remains limited. Development of highly potent and selective small-molecule MIF inhibitors and validation of their use in relevant disease models will advance drug discovery. In this review, we provide an overview of recent advances in the identification of MIF as a pharmacological target in the pathogenesis of inflammatory diseases and cancer. We also give an overview of the current developments in the discovery and design of small-molecule MIF inhibitors and define future aims in this field.

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Conflict of interest statement

Conflict of Interest

The authors declare that they have no conflict of interest.

Figures

Figure 1
Figure 1
A. Crystal structure of MIF, showing that three monomers associate to form a symmetrical homotrimer (PDB 1CA7), B. MIF catalyses the tautomerisation of α-keto-carboxylates, C. Diseases for which a role of MIF has been described.
See this image and copyright information in PMC

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