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Small-molecule inhibitors of macrophage migration inhibitory factor (MIF) as an emerging class of therapeutics for immune disorders
Drug Discovery Today ( IF 6.5 ) Pub Date : 2018-06-21 , DOI: 10.1016/j.drudis.2018.06.017
Tjie Kok 1 , Anna A Wasiel 2 , Robbert H Cool 2 , Barbro N Melgert 3 , Gerrit J Poelarends 2 , Frank J Dekker 2
Affiliation  

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.



中文翻译:

巨噬细胞迁移抑制因子 (MIF) 的小分子抑制剂作为一类新兴的免疫疾病疗法

巨噬细胞迁移抑制因子 (MIF) 是一种重要的细胞因子,在炎症和癌症的发病机制中描述了其越来越多的功能。然而,在相关疾病模型中得到充分表征的强效药物样 MIF 抑制剂的可用性仍然有限。开发高效和选择性的小分子 MIF 抑制剂并验证它们在相关疾病模型中的使用将推动药物发现。在这篇综述中,我们概述了 MIF 作为炎症疾病和癌症发病机制中的药理学靶点的最新进展。我们还概述了小分子 MIF 抑制剂的发现和设计的当前发展,并定义了该领域的未来目标。

更新日期:2018-06-21
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