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首页> 外文期刊>Future medicinal chemistry >Quercetin/oleic acid-based G-protein-coupled receptor 40 ligands as new insulin secretion modulators
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Quercetin/oleic acid-based G-protein-coupled receptor 40 ligands as new insulin secretion modulators

机译:基于槲皮素/油酸的G蛋白偶联受体40配体作为新的胰岛素分泌调节剂

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摘要

Aim: Management of Type 2 diabetes mellitus by diet is achievable at the early stage of the disease; patients usually underestimate this approach and an appropriate drug therapy is required. Results: Starting from quercetin and oleic acid, that have effect on insulin secretion, a small set of hybrid molecules was synthesized. Insulin secretion was evaluated in both in vitro and ex vivo models. AV1 was able to enhance insulin secretion dose dependently, behaving as a conceivable agonist of G-protein-coupled receptor 40. Conclusion: AV1 represents an interesting tool that interacts with G-protein-coupled receptor 40. Further studies will be carried out to evaluate the exact binding mode, and also to enlarge the library of these antidiabetic agents.
机译:目的:在疾病的早期阶段可实现2型糖尿病患者的糖尿病; 患者通常低估这种方法和需要适当的药物治疗。 结果:从槲皮素和油酸开始,对胰岛素分泌有影响,合成了一小组杂化分子。 在体外和离体模型中评估胰岛素分泌。 AV1能够依赖地增强胰岛素分泌剂量,表现为G蛋白偶联受体40的可想象激动剂。结论:AV1代表与G蛋白偶联受体40相互作用的有趣工具。将进行进一步的研究以评估 确切的结合模式,以及扩大这些抗糖尿病药剂的文库。

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