酪氨酸蛋白磷酸酯酶1B抑制剂的构效关系

Structure-activity Relationship of Protein Tyrosine Phosphatase 1B Inhibitors

介绍了最近几年来关于酪氨酸蛋白磷酸酯酶1B作用的机制以及通过各种途径发现的结构新颖的小分子抑制剂的构效关系研究进展。酪氨酸蛋白磷酸酯酶1B在胰岛素依赖的信号传导途径中发挥着非常重要的作用,并作为一个潜在的治疗2型糖尿病和肥胖的作用靶点日益受到广泛的关注。在其晶体结构被报道后,强效和选择性好的抑制剂更成为研制开发新药的焦点。

The advances made in the new compounds identified as Protein Tyrosine Phosphatases 1B （PTP1 B） inhibitors recently and their structure-activity relationship were reviewed in this paper. PTP1B plays a very important role in the insulin-dependent signaling cascade and has attracted considerable attention as a possible target for the treatment of type 2 diabetes and obesity. After its crystal structure was reported, much effort has been made to search for the potent and selective inhibitors.