G protein–coupled receptors (GPCRs) continue to be important discovery targets for the treatment of type 2 diabetes mellitus (T2DM). Many GPCRs are directly involved in the development of insulin resistance and β-cell dysfunction, and in the etiology of inflammation that can lead to obesity-induced T2DM. This review summarizes the current literature describing a number of well-validated GPCR targets, but also outlines several new and promising targets for drug discovery. We highlight the importance of understanding the role of these receptors in the disease pathology, and their basic pharmacology, which will pave the way to the development of novel pharmacological probes that will enable these targets to fulfill their promise for the treatment of these metabolic disorders.

中文翻译：

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G蛋白偶联的受体，靶向胰岛素抵抗，肥胖和2型糖尿病

G蛋白偶联受体（GPCR）仍然是治疗2型糖尿病（T2DM）的重要发现目标。许多GPCR直接参与胰岛素抵抗和β细胞功能障碍的发展，以及可能导致肥胖引起的T2DM的炎症病因。这篇综述总结了描述许多经过良好验证的GPCR靶标的最新文献，同时也概述了用于药物发现的几个新的有希望的靶标。我们强调了解这些受体在疾病病理学中的作用及其基本药理学的重要性，这将为新型药理探针的开发铺平道路，这将使这些靶标能够实现其对这些代谢性疾病的治疗。