G蛋白偶联受体
食欲
2型糖尿病
肥胖
糖尿病
能量稳态
医学
生物信息学
葡萄糖稳态
生物
受体
胰岛素抵抗
内分泌学
内科学
作者
Sebastian G.B. Furness,Noah Piper,Emily A. Whitfield,Gregory D. Stewart,Xiaomeng Xu
标识
DOI:10.1016/j.bcp.2022.115115
摘要
Type 2 diabetes and obesity have reached pandemic proportions throughout the world, so much so that the World Health Organisation coined the term "Globesity" to help encapsulate the magnitude of the problem. G protein-coupled receptors (GPCRs) are highly tractable drug targets due to their wide involvement in all aspects of physiology and pathophysiology, indeed, GPCRs are the targets of approximately 30% of the currently approved drugs. GPCRs are also broadly involved in key physiologies that underlie type 2 diabetes and obesity including feeding reward, appetite and satiety, regulation of blood glucose levels, energy homeostasis and adipose function. Despite this, only two GPCRs are the target of approved pharmaceuticals for treatment of type 2 diabetes and obesity. In this review we discuss the role of these, and select other candidate GPCRs, involved in various facets of type 2 diabetic or obese pathophysiology, how they might be targeted and the potential reasons why pharmaceuticals against these targets have not progressed to clinical use. Finally, we provide a perspective on the current development pipeline of anti-obesity drugs that target GPCRs.
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