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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Receptor agonists of macrophage migration inhibitory factor.
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Receptor agonists of macrophage migration inhibitory factor.

机译:巨噬细胞迁移抑制因子的受体激动剂。

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摘要

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.
机译:细胞因子MIF通过其与跨膜受体CD74结合而引发的途径参与炎症和细胞增殖。 MIF还促进AMPK激活,对心肌梗塞和局部缺血/再灌注反应有潜在益处。基于结构的分子设计不仅导致发现拮抗剂,而且还发现了MIF-CD74结合的第一个激动剂。这些化合物包含三唑核心,该核心很容易通过铜催化的点击化学进行组装。通过研究人类成纤维细胞中MIF依赖的ERK1 / 2磷酸化,证实了激动剂和拮抗剂的行为。

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