G‐protein‐coupled receptors (GPCRs) respond to various physiological ligands such as photons, ions, and small molecules that include amines, fatty acids, and amino acids to peptides, proteins and steroids. Therefore, this family of proteins represents an attractive target for biopharmaceutical research [1]. The physiological role of fatty acids and other lipid molecules as important signal mediators is well studied in various metabolic pathways [2]. Acute administration of free fatty acids (FFAs) stimulates insulin release. Conversely, chronic exposure to high levels of free fatty acids leads to impairment of β cell function and lipotoxicity. However, the receptors through which these fatty acids and lipids act were unknown, until the identification of fatty acid binding receptors: GPR40, GPR41, GPR43, and GPR119. Based on their tissue‐expression profile, and pharmacologic analysis, the fatty acid binding receptors along with lipid binding receptor GPR119 are linked to diabetes and obesity. They play a critical role in the metabolic regulation of insulin release and glucose homeostasis. In this review, the mechanism of receptor activation, pharmacology, and the physiological functions of the fatty acid binding receptors will be discussed.

中文翻译：

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脂肪酸结合受体及其在 2 型糖尿病中的生理作用

G 蛋白偶联受体 (GPCR) 对各种生理配体（如光子、离子和小分子（包括胺、脂肪酸和氨基酸）、肽、蛋白质和类固醇）作出反应。因此，该蛋白质家族代表了生物制药研究的一个有吸引力的目标 [1]。脂肪酸和其他脂质分子作为重要信号介质的生理作用在各种代谢途径中得到了很好的研究 [2]。游离脂肪酸 (FFA) 的急性给药会刺激胰岛素释放。相反，长期暴露于高水平的游离脂肪酸会导致 β 细胞功能和脂毒性受损。然而，在脂肪酸结合受体 GPR40、GPR41、GPR43 和 GPR119 被鉴定之前，这些脂肪酸和脂质通过哪些受体起作用是未知的。根据它们的组织表达谱和药理学分析，脂肪酸结合受体和脂质结合受体 GPR119 与糖尿病和肥胖有关。它们在胰岛素释放和葡萄糖稳态的代谢调节中起关键作用。在这篇综述中，将讨论受体激活的机制、药理学和脂肪酸结合受体的生理功能。