Receptor agonists of macrophage migration inhibitory factor
Receptor agonists of macrophage migration inhibitory factor
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DOI：
10.1016/j.bmcl.2010.09.118
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发表时间：
2010-12-01
影响因子：
2.7
通讯作者：
Bucala, Richard
中科院分区：
文献类型：
--
作者：
Jorgensen, William L.;Gandavadi, Sunilkumar;Bucala, Richard
细胞因子MIF通过与跨膜受体CD 74结合启动的途径参与炎症和细胞增殖。MIF还促进AMPK激活，对应对心肌梗死和缺血再灌注有潜在益处。基于结构的分子设计不仅发现了MIF-CD 74结合的拮抗剂，而且发现了MIF-CD 74结合的第一个激动剂。所述化合物含有三唑核，所述三唑核容易通过Cu催化的点击化学组装。通过研究人成纤维细胞中MIF依赖性ERK 1/2磷酸化来证实激动剂和拮抗剂行为。(C)2010爱思唯尔有限公司版权所有。
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. (C) 2010 Elsevier Ltd. All rights reserved.