Department of Medicine, Surgery and Neurosciences, University of Siena, Italy; Fondazione Umberto Di Mario ONLUS c/o Toscana Life Science, Siena, Italy.
Department of Medicine, Surgery and Neurosciences, University of Siena, Italy.
Best Pract Res Clin Endocrinol Metab. 2018 Apr;32(2):201-213. doi: 10.1016/j.beem.2018.02.005. Epub 2018 Mar 15.
G-protein coupled receptors (GPCRs) represent the largest receptor family in the genome and are of great interest for the design of novel drugs in a wide variety of diseases including neurologic disorders, obesity and Type 2 diabetes mellitus. The latter is a chronic disease characterized by insulin resistance and impaired insulin secretion, affecting >400 million patients worldwide. Here we provide an overview on: a) The molecular basis of GPCR signalling and of its involvement in the regulation of insulin secretion and of glucose homeostasis; b) the role of GPCRs in type 2 diabetes pathophysiology and as therapeutic targets of current and future glucose-lowering drugs.
G 蛋白偶联受体 (GPCRs) 是基因组中最大的受体家族，它们在治疗多种疾病（包括神经紊乱、肥胖和 2 型糖尿病）方面的新药设计中具有重要的应用价值。后者是一种慢性疾病，其特征为胰岛素抵抗和胰岛素分泌受损，影响全球超过 4 亿患者。在此，我们概述了：a）GPCR 信号转导的分子基础及其在胰岛素分泌和葡萄糖稳态调节中的作用；b）GPCRs 在 2 型糖尿病病理生理学中的作用，以及作为当前和未来降血糖药物的治疗靶点。
