选择性PPARγ调节剂治疗2型糖尿病的研究

Studies on Selective PPARγ Modulators Antidiabetic Agents in the Treatment of Type 2 Diabetes

综述已上市的噻唑二烷酮类胰岛素增敏剂作为过氧化物酶体增殖因子激活受体γ(PPARγ)激动剂治疗2型糖尿病的疗效及安全性,并介绍正处于开发阶段的选择性PPARγ调节剂(或部分激动剂)及其三维定量构效关系和药效团的研究。PPARγ是一类位于细胞核内由配体调节的核激素受体,被激动剂激活以后,可以增强胰岛素敏感性。而选择性PPARγ调节剂能有效增强胰岛素敏感性且减少激动剂所产生的副作用,已成为治疗2型糖尿病药物研究的一个新方向。

The curative effect and safety of launched thiazolidinedions （TZDs）, insulin-sensitizers, as peroxisome proliferators activated receptor γ（PPARγ） agonists in the treatment of type 2 diabetes were reviewed, and here the recent studies on selective PPARγ modulators （or partial agonists） in development and their 3D-QSAR and pharmacophores were presented. PPARγ is a very important ligand-activated nuclear hormone receptor in cell. Activated by agonists, the receptor plays a crucial role in glucose utilization and insulin sensitization. The research and development of novel selective PPARγ modulators that retain efficacious insulin-sensitizing properties while minimizing potential adverse side effects as type 2 diabetes drugs have become a new direction and tendency.