G-protein coupled receptor 40 agonists as novel therapeutics for type 2 diabetes
G-protein coupled receptor 40 agonists as novel therapeutics for type 2 diabetes
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DOI：
10.1007/s12272-013-0283-3
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发表时间：
2014-04-01
影响因子：
6.7
通讯作者：
Lee, Ju-Yeun
中科院分区：
文献类型：
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作者：
Choi, Yun Jung;Shin, Dongyun;Lee, Ju-Yeun
随着对单独或与现有药物联合应用安全有效的新型抗糖尿病药物的需求日益增加，G蛋白偶联受体40(GPR40)作为治疗2型糖尿病的潜在靶点已引起人们的广泛关注。因为GPR40激动剂可能通过作用于环境中的葡萄糖依赖方式而提供常用药物的优势，这种方式机械地导致降低发生低血糖的风险。自从2003年去孤构化以来，小分子GPR40激动剂的开发受到了几个研究小组的推动。有许多靶向GPR40的先导分子，其中TAK-875(完全激动剂)和AMG837(部分激动剂)进入临床阶段。
With growing needs for new antidiabetic drugs which are safe and effective alone or in combination with existing drugs, G-protein coupled receptor 40 (GPR40) has drawn a considerable attention as a potential therapeutic target for type 2 diabetes. As GPR40 agonist may offer advantages to commonly used agents, by acting ambient glucose dependent manner which mechanistically leads to reduced risk of developing hypoglycemia. Since deorphanization in 2003, development of small molecule GPR40 agonists has been spurred by several research groups. There are a number of lead molecules targeting GPR40, and among these molecules TAK-875 (full agonist) and AMG 837 (partial agonist) advanced into clinical stage.