摘要
2型糖尿病表现为糖脂代谢紊乱并伴随多脏器慢性损害,已成为威胁人类健康的巨大隐患。α/β水解酶结构域-6(α/βhydrolase domain-6,ABHD6)通过水解单酰甘油,负调控胰岛素的释放。小分子ABHD6抑制剂因其在增强胰岛素敏感性、改善脂肪功能等方面的重要作用而有望成为新一代治疗2型糖尿病的药物。本文介绍了ABHD6的作用机制,根据其结构特点对此类抑制剂的最新研究进展进行综述,并对其构效关系进行分析。
Type 2 diabetes, a glucose and lipid metabolism disorder accompanied by chronic multiple organ damage, has become a huge threat to human health. α/β hydrolase domain-6(ABHD6)regulates the insulin release negatively by hydrolyzing monoacylglycerol. Small molecule ABHD6 inhibitors have been proven to lower blood-glucose and regulates energy homeostasis, which is a potential candidate for the treatment of type 2 diabetes. This paper introduced the ABHD6 signaling pathway and its mechanism, then reviewed the progress of small molecule ABHD6 inhibitors with different structures in recent years, and analyzed the structure activity relationship.
keywords:glucose and lipid metabolism α/β hydrolase domain-6 ABHD6 inhibitors antidiabetic drugs advances
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2017年第2期125-134,共10页
Journal of China Pharmaceutical University