摘要
钠-葡萄糖协同转运蛋白(SGLTs)主要存在于小肠黏膜(SGLT1)和肾近曲小管(SGLT1和SGLT2)的转运基因家族,其表达的膜蛋白负责将葡萄糖、氨基酸、维生素、离子和渗透溶质转运至肾近曲小管的刷状缘细胞及小肠上皮细胞。而SGLT2是一种主要在肾脏特异性表达的高效能-低亲和力转运体。葡萄糖在肾近曲小管的重吸收约有90%由SGLT2完成,因此选择性地阻断SGLT2、减少重吸收、增加尿糖排出这一治疗策略已成为糖尿病领域的又一创新性研究,为糖尿病治疗药物提供了新作用靶点。本文对SGLT2抑制剂在治疗2型糖尿病方面的最新研究进展进行介绍,主要阐述其作用机制、疗效(部分在研SGTL2抑制剂的临床试验结果)和安全性。
Sodium-glucose co-transporters （SGLT） are a family of glucose transporter chiefly exist in the intestinal mucosa of the small intestine （SGLT1） and theproximal tubule of the nephron （SGLT1 and SGLT2）, the membrane protein SGLT expressed are responsible for the transport of glucose, amino acids, vitamins, ions and osmolytes across the brush-border membrane of proximal renal tubules as well as the intestinal epithelium. SGLT2 is a high-capacity, low-affinity transporter which is specifically expressed in the kidney. It accounts for approximately 90% of glucose reabsorption in the proximal tubules. So, studies on selectively block the SGLT2 that leading to less glucose reabsorption and increased glucosuria are creative. SGLT2 inhibitors is also recognized as a new antidiabetic drug. In this paper, the latest research progress on SGLT2 inhibitor for the treatment of type 2 diabetes were reviewed. The mechanism, therapeutic effect （the data of clinical trials under research and development） and the safety of of SGLT2 inhibitor were introduced.
出处
《药品评价》
CAS
2010年第17期18-21,共4页
Drug Evaluation
