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新型抗2型糖尿病药物钠-葡萄糖协同转运蛋白2抑制剂研究进展 被引量：9

Progress in sodium-glucose co-transporter-2 inhibitors:new drugs for treatment of type 2 diabetes
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摘要 钠-葡萄糖协同转运蛋白(SGLT)是一类位于小肠黏膜(SGLT1)和肾近曲小管(SGLT2和SGLT1)中的葡萄糖转运基因家族。其中,SGLT2是一种低亲和力的转运蛋白,在肾脏中特异性表达并且在近曲小管葡萄糖重吸收中发挥非常重要的作用。它可以选择性地抑制SGLT2,即可通过增加尿糖的排出来治疗2型糖尿病,是一种创造性的治疗策略。本文介绍了SGLT2抑制剂在2型糖尿病治疗研究方面的最新进展,重点综述了SGLT2抑制剂的作用机制、部分在研SGLT2抑制剂的生物活性数据及临床试验结果。 Sodium-glucose co-transporters（SGLT） are a family of glucose transporter found in the intestinal mucosa of the small intestine（SGLT1） and the proximal tubule of the nephron（SGLT1 and SGLT2）.The sodium-glucose co-transporter-2（SGLT2） is a low-affinity transporter that is specifically expressed in kidney and plays a very important role in renal glucose reabsorption in the proximal tubule.Selective inhibition of SGLT2 is an innovative therapeutic strategy for the treatment of type 2 diabetes by en-hancing glucose loss through urine.In this paper,the latest research progress on SGLT2 inhibitors for the treatment of type 2 diabetes was introduced.We emphasized the mechanism of SGLT2 inhibitors,the data of biological activities and clinical trials of some SGLT2 inhibitors under research and development.
作者 张富东 李玲
机构地区 昆明医学院云南省天然药物重点实验室
出处 《国际药学研究杂志》 CAS 2011年第5期375-380,共6页 Journal of International Pharmaceutical Research
关键词 2型糖尿病 药物治疗 钠-葡萄糖协同转运蛋白 抑制剂 type2 diabetes drug therapy sodium-glucose co-transporters（SGLT） Inhibitors
分类号 R96 [医药卫生—药理学]
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参考文献27

  • 1Meng W,Ellsworth BA,Nirschl AA,et al.Discovery of dapagliflozin:a potent,selective renal sodium-dependent glucose cotransporter 2 (SGLT2)inhibitor for the treatment of type 2 diabetes[J].J Med Chem,2008,51(5):1145-1149.
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同被引文献73

  • 1吕书红,李曼春,田本淳,鲍科臻,江军.实施糖尿病社区管理模式前后患者社区卫生服务利用的意愿调查[J].中国全科医学,2006,9(11):915-916. 被引量：4
  • 2Koro C E,Bowlin S J,Bourgeois N,et al.Glycemic control from 1988 to 2000 among U.S.adults diagnosed with type 2 diabetes:a preliminary report[J].Diabetes Care,2004,27(1):17-20.
  • 3Hediger M A,Rhoads D B.Molecular physiology of sodium glucose cotransporters[J].Physiol Res,1994,74(4):993-1026.
  • 4William N W.Development of the renal glucose reabsorption inhibitors:A new mechanism for the pharmacotherapy of diabetes mellitus type 2[J].J Med Chem,2009,52(7):1785-1794.
  • 5Kipnes M S.Sodium-glucose cotransporter 2 inhibitors in the treatment of type 2 diabetes:a review of phase II and III trials[J].Clin Invest,2011,1(1):145-156.
  • 6Ehrenkranz J R L,Lewis N G,Kahn C R.Phlorizin:a review[J].Diabetes Metab Res Rev,2005,21(1):31-38.
  • 7Oku A,Ueta K,Arakawa K.T-1095,an inhibitor of renal Na+-glucose cotransporters,may provide a novel approach to treating diabetes[J].Diabetes,1999,48(9):1794-1800.
  • 8Ueta K,Ishihara T,Matsumoto Y.Long-term treatment with the Na+-glucose cotransporter inhibitor T-1095 causes sustained improvement in hyperglycemia and prevents diabetic neuropathy in Goto-Kakizaki rats[J].Life Sci,2005,76(23):2655-2668.
  • 9Boldys A,Okopien B.Inhibitors of type 2 sodium glucose cotransporters——a new strategy for diabetes treatment[J].Pharmacol Rep,2009,61(5):778-784.
  • 10Katsuno K,Fujimori Y,Takemura Y.Sergliflozin,a novel selective inhibitor of low-affinity sodium glucose cotransporter(SGLT2),validates the critical role of SGLT2 in renal glucose reabsorption and modulates plasma glucose level[J].Pharmacol Exp Ther,2007,320(1):323-330.

引证文献9

二级引证文献37

国际药学研究杂志
2011年 第5期

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