Tiwari Atul
Jubilant Biosys Ltd, Drug Discovery Unit, Metabolic Disorder Lab, 96, 2nd Stage, Industrial Suburb, Yeshwantpur, Bangalore, Karnatka, 560022, India.
Curr Opin Investig Drugs. 2010 Apr;11(4):385-93.
A new role for fatty acids as endocrine regulators of lipid and carbohydrate metabolism through the activation of their cognate receptors, GPCRs, has been discovered during the past decade. GPR43 is a GPCR that has been implicated in the regulation of fatty-acid and glucose homeostasis in adipose tissue and the intestines, thus having potential therapeutic relevance in the treatment of type 2 diabetes, insulin resistance and obesity. Ongoing drug discovery efforts are focused toward the development of a novel, potent and selective orthosteric or allosteric modulator that acts as an agonist for GPR43. This review summarizes data supporting a role for GPR43 in the pharmacological management of metabolic disorders.
在过去十年中，人们发现了脂肪酸作为脂质和碳水化合物代谢的内分泌调节剂的新作用，其通过激活同源受体G蛋白偶联受体（GPCR）来实现。GPR43是一种GPCR，与脂肪组织和肠道中脂肪酸和葡萄糖稳态的调节有关，因此在2型糖尿病、胰岛素抵抗和肥胖症的治疗中具有潜在的治疗意义。正在进行的药物研发工作集中在开发一种新型、强效且选择性的正构或变构调节剂，作为GPR43的激动剂。本综述总结了支持GPR43在代谢紊乱药物治疗中作用的数据。
