PTP1B抑制剂抗糖尿病作用的研究进展

Research progress of PTP1B inhibitors for the treatment of diabetes

糖尿病是目前世界范围内严重威胁人类健康的慢性疾病之一,常伴有严重的临床并发症,如糖尿病性心肌病、肾病、视网膜病变、神经病变等。2型糖尿病(type 2 diabetes mellitus,T2DM)是最常见的糖尿病类型,其发展受到多种遗传因素和环境因素影响。蛋白酪氨酸磷酸酶1B(protein tyrosine phosphatase 1B,PTP1B)在胰岛素信号转导通路负调控中发挥重要作用,已成为治疗2型糖尿病(diabetes mellitus type 2,T2DM)和肥胖症的有效靶点,探索高效安全的PTP1B抑制剂受到越来越多的关注,本文作者以PTP1B酶与T2DM和肥胖症的关系为基础,归纳整理了近年来国内外PTPIB治疗糖尿病的相关文献,综述了PTP1B抑制剂包括天然产物,天然产物衍生物,合成小分子的研究进展,旨在为设计靶向抑制PTP1B的抗糖尿病和肥胖药物的开发提供思路。

Diabetes mellitus is one of the chronic diseases that threaten human health in the world.It is often accompanied by serious clinical complications,such as diabetic cardiomyopathy,nephropathy,retinopathy,neuropathy,etc.Type 2 diabetes mellitus(T2DM)is the most common type of diabetes,and its development is influenced by a variety of genetic and environmental factors.Protein tyrosine phosphatase 1B(PTP1B)plays an important role in the negative regulation of the insulin signal transduction pathway and has become an effective target for the treatment of type 2 diabetes(T2DM)and obesity.Texploration of highly effective and safe PTP1B inhibitors is getting more and more attention.Based on the relationship between PTP1B enzyme and T2DM and obesity,the authors summarized the relevant literatures on the treatment of diabetes mellitus by PTPIB inhibitors in recent years,and reviewed the research progress of PTP1B inhibitors including natural products,natural product derivatives and synthetic small molecules.The aim is to provide ideas for the development of anti-diabetes and obesity drugs with targeted inhibition of PTP1B.