| 引用本文: | 陈福欣,龚频,周安宁.基于SGLT2受体蛋白的新型糖尿病药物的研究进展[J].中国现代应用药学,2012,29(8):687-692. |
| CHEN Fuxin,GONG Pin,ZHOU Anning.Progress Research on Novel Anti-Diabetes Drugs Based on SGLT2 Receptor Protein[J].Chin J Mod Appl Pharm(中国现代应用药学),2012,29(8):687-692. |
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| 摘要: |
| 目的 钠-葡萄糖共转运蛋白2(SGLT2)是肾小管上负责将尿糖重新吸收为血糖的重要转运蛋白，对该蛋白的抑制可以使糖从血液中转移进入尿液。本文总结了目前各大药物公司在研的SGLT2抑制剂的构效关系及其临床研究进展。方法 综述了近年来国内外相关报道，对O,C,N-糖甙类和非糖苷类SGLT2抑制剂的药理、药效和药代学进行讨论，并就其临床研究及开发上市状况进行概述。结果 SGLT2抑制剂的结构与其药理活性和代谢稳定性间的关系是该类药物研发的重点。结论 SGLT2抑制剂与降糖作用的构效关系，对开发新一代治疗糖尿病药物具有重要意义。 |
| 关键词: 二型糖尿病 SGLT2 转运蛋白 降糖 |
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| 基金项目:西安科技大学博士启动基金(A5031018，2010020) |
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| Progress Research on Novel Anti-Diabetes Drugs Based on SGLT2 Receptor Protein |
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CHEN Fuxin1, GONG Pin2, ZHOU Anning1
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1.Department of Chemistry and Chemical Engineering, Xi’an University of Science and Technology, Xi’an 710054, China;2.College of Life Science and Engineering, Shaanxi University of Science and Technology, Xi’an 710021, China
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| Abstract: |
| OBJECTIVE Sodium-dependent glucose cotransporter 2(SGLT2) is the important transporter protein on renal tubules which is responsible for the re-absorbance of urine glucose to blood glucose. This review summaries various of SGLT2 inhibitors and emphasis on the SAR and clinical research. METHODS According to the correlative reports in recent years, various of SGLT2 inhibitor, including O-glycoside, C-glycoside, N-glycoside and non-glycoside were discussed about their pharmacology pharmacodynamics and pharmacokinetics. RESULTS It was important for the drug’s R&D to identify the relationship between the structure of inhibitors and their activity and metabolic stability. CONCLUSION It is essential to grasp the SAR of SGLT2 inhibitor and their hypoglycemic effect for the discovery of new generation diabetes drugs. |
| Key words: diabetes mellitus type 2 SGLT2 cotransport protein hypoglycemic agents |
