...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Canadian Journal of Physiology and Pharmacology >Discovery of ethyl urea derivatives as inhibitors of islet amyloid polypeptide fibrillization and cytotoxicity
【24h】

Discovery of ethyl urea derivatives as inhibitors of islet amyloid polypeptide fibrillization and cytotoxicity

机译：发现乙基脲衍生物作为胰岛淀粉样蛋白多肽纤维化和细胞毒性的抑制剂

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Islet amyloid polypeptide (IAPP) has been shown to form amyloid deposits in pancreatic islets, thereby furthering type 2 diabetes disease progression. Further discovery of new molecules is needed to create a diverse set of molecules that impede pancreatic amyloidosis. We have recently designed and synthesized N-phenyl-N'-(2-ethyl)ureas (EU) that are non-cytotoxic small molecules, to evaluate the role of the aryl-substituted moiety on the inhibition of hIAPP fibrillization. Several EUs were tested in vitro for their anti-amyloidogenic activity using the fluorometric ThT assay, the photo-induced cross-linking (PIUCP) assay, and cell survival assay in pancreatic MIN-6 cells. EU-362 and EU-418 were able to significantly inhibit the formation of hIAPP fibrils and protected cells from amyloid cytotoxic effects. Our results suggest that increasing the nucleophilic potency of the aryl moiety significantly enhances the anti-amyloidogenic activity of the molecules.
机译：已经证明了胰岛淀粉样蛋白多肽（IAPP）在胰岛胰岛中形成淀粉样液，从而进一步进行2型糖尿病疾病进展。 需要进一步发现新分子以产生妨碍胰腺淀粉样蛋白病的各种分子。 我们最近设计和合成的N-苯基-N' - （2-乙基）脲（EU），其是非细胞毒性的小分子，以评估芳基取代部分对HIAPP纤维化抑制作用的作用。 使用荧光THT测定，光学诱导的交联（PIUCP）测定和胰MIN-6细胞中的光学诱导的交联（PIUCP）测定和细胞存活测定，在体外测试几种EUS。 EU-362和EU-418能够显着抑制HIAPP原纤维的形成和来自淀粉样蛋白细胞毒性作用的保护细胞。 我们的研究结果表明，增加芳基部分的亲核效力显着提高了分子的抗淀粉样蛋白活性。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号