The high level of expression in pancreatic beta cells and the dependence of the glucose to stimulate the secretion of insulin make theGPR40 an interesting target for treatment of type 2 diabetes. The development of novel agonists of this receptor is a hot topic in Medicinal Chemistry. Herein, we describe a review on the structure–activity relationships of GPR40 agonists focusing on the main strategies of medicinal chemistry used to develop each one of the main structural patterns exploited for this purpose, and we provide a general model for the design of novel GPR40 ligands.

中文翻译：

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对游离脂肪酸受体1（FFA1R或GPR40）的激动剂作用的结构基础

胰腺β细胞中的高水平表达和葡萄糖对胰岛素分泌的依赖性使GPR40成为治疗2型糖尿病的有趣靶标。该受体的新型激动剂的开发是药物化学中的热门话题。在这里，我们描述了GPR40激动剂的结构-活性关系的综述，重点是用于开发用于此目的的每种主要结构模式的药物化学的主要策略，并为新型GPR40的设计提供了通用模型配体。