巨噬细胞移动抑制因子受体激动剂。
Receptor agonists of macrophage migration inhibitory factor.
机构信息
Department of Chemistry, Yale University, New Haven, CT 06520, USA.
出版信息
Bioorg Med Chem Lett. 2010 Dec 1;20(23):7033-6. doi: 10.1016/j.bmcl.2010.09.118. Epub 2010 Sep 29.
Abstract
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.
摘要
细胞因子 MIF 通过与其跨膜受体 CD74 结合所引发的途径参与炎症和细胞增殖。MIF 还促进 AMPK 的激活，这可能有益于对心肌梗死和缺血再灌注的反应。基于结构的分子设计不仅导致了 MIF-CD74 结合的拮抗剂的发现，而且还导致了其第一个激动剂的发现。这些化合物含有一个三唑核心，可通过 Cu 催化的点击化学轻松组装。通过研究人成纤维细胞中 MIF 依赖性 ERK1/2 磷酸化，证实了激动剂和拮抗剂的行为。
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本文引用的文献
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