Diabetes Research Group, Division of Diabetes & Nutritional Sciences, King's College London, UK.
Curr Opin Pharmacol. 2017 Dec;37:24-28. doi: 10.1016/j.coph.2017.08.001. Epub 2017 Aug 17.
The incidence of type 2 diabetes (T2D) is increasing at an alarming rate, which is imposing substantial healthcare and economic burdens worldwide. T2D can be treated by a range of drugs, but there is a need to identify additional therapeutic options. Human islets express nearly three hundred G-protein-coupled receptors (GPCRs), which could be targeted for the treatment of T2D. However, to date, the GLP-1 receptor is the only islet GPCR for which agonists are in current clinical use. This review explores pharmaceutical development of drugs that activate individual or multiple β-cell GPCRs and explains how our knowledge of GPCR expression by human islets may inform direction on novel GPCR targets.
2 型糖尿病（T2D）的发病率正在以惊人的速度增长，给全球的医疗保健和经济带来了巨大的负担。T2D 可以通过一系列药物来治疗，但需要确定更多的治疗选择。人类胰岛表达近三百种 G 蛋白偶联受体（GPCR），这些受体可以作为治疗 T2D 的靶点。然而，迄今为止，GLP-1 受体是唯一一种用于临床的胰岛 GPCR 激动剂。这篇综述探讨了激活单个或多个β细胞 GPCR 的药物的药物研发，并解释了我们对人类胰岛 GPCR 表达的了解如何为新的 GPCR 靶点提供方向。
