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作为2型糖尿病治疗药物的G蛋白偶联受体40激动剂研究进展 被引量:1

Recent Research Advances in G-protein Coupled Receptor 40 Agonists as Therapeutic Agents for Type 2 Diabetes
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摘要 2型糖尿病约占糖尿病总病例数的90%,目前研发的其新型治疗药物主要是通过调节糖代谢通路来控制血糖水平,它们可通过激活G蛋白偶联受体尤其是G蛋白偶联受体40,增强胰岛β细胞功能,促进胰岛素分泌,提高机体对胰岛素的敏感性,从而达到治疗糖尿病的目的。G蛋白偶联受体40作为抗2型糖尿病的新靶点,以其潜在优势,在糖尿病治疗领域备受关注。简介G蛋白偶联受体与其配体游离脂肪酸,重点综述不同结构的G蛋白偶联受体40激动剂的研究进展。 Type 2 diabetes accounts for about 90% of all eases of diabetes. Novel therapeutic drugs for type 2 diabetes in current research and development control blood glucose level mainly by regulating glycometabolism pathways, which could strengthen the function of islet beta cells, promote insulin secretion and improve the body's sensitivity to insulin through activating G-protein coupled receptors(GPRs), especially GPR40, so as to achieve the goal of treating diabetes. GPR40 as novel therapeutic targets for type 2 diabetes, with its potential advantages, has attracted much attention in the field of diabetes treatment. GPRs and Their ligands -free fatty acids were Introduced. The research progress on GPR40 agonists with different structures was especially reviewed.
出处 《药学进展》 CAS 2015年第1期13-22,共10页 Progress in Pharmaceutical Sciences
基金 国家"重大新药创制"科技重大专项(No.2013ZX09301303-002) 江苏省自然科学基金(No.BK 20141349)
关键词 G蛋白偶联受体40 激动剂 2型糖尿病 胰岛素分泌 血糖水平 GPR40 agonist type 2 diabetes insulin secretion blood glucose level
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  • 1Wild S, Roglic G, Green A, et al. Global prevalence of diabetes:estimates for the year 2000 and projections for 2030[J]. Diabetes Care,2004, 27(5): 1047-1053. 被引量:1
  • 2Vassilatis D K. Hohmann J G, Zeng H, et al. The G protein-coupledrcccptor repertoires of human and mouse[J]. Proc Nall Acad Sci USA,2003, 100(8): 4903-4908. 被引量:1
  • 3Ellis C, Smith A. Highlighting the pitfalls and possibilities of drugrcscarch[J], Nat Rev Drug Discov, 2004, 3(3): 238-278. 被引量:1
  • 4Kebede M A, Alquicr T, Latour M G, et al. Lipid receptors and isletfunction: therapeutic implications?[J]. Diabetes Obes Metab, 2009, 11(Suppl4): 10-20. 被引量:1
  • 5Inscl P A, Tang C M, Hahntow I, et al. Impact of GPCRs in clinicalmedicine: monogenic diseases, genetic variants and drug targets[J].Biochim Biophvs Acta, 2007, 1768(4): 994-1005. 被引量:1
  • 6Schmitz G, Ecker J. The opposing effects of n-3 and n-6 fatly acids [J].Prog Lipid Res, 2008, 47(2): 147-155. 被引量:1
  • 7Miyauchi S, Hirasawa A, Ichimura A, et al. New frontiers in gut nutrientsensor research: free fatty acid sensing in the gaslrointestinal tractfj]. JPharmacol Sci, 2010, 112(1): 19-24. 被引量:1
  • 8Sauer L A, Dauchy R T, Blask D E. Mechanism tor the antitumor andanlicachcctic effects of n-3 fatty acids[J]. Cancer Res,2000,60(18):5289-5295. 被引量:1
  • 9Louct J F, Chatclain F, Decaux J F, et al. Long-chain fatly acids regulateliver camitinc palmitoyltransferase I gene (L-CPT I) expression througha pcroxisome-proliferator-activated receptor alpha (PPARalpha)-indcpcndent pathway[J]. Biochem J, 2001, 354(Pt 1): 189-197. 被引量:1
  • 10Xiong Y, Miyamoto N, Shibata K, et al. Short-chain fatly acids stimulateleptin production in adipocytes through ihe G protein-coupled receptorGPR41[J]. Proc Natl Acad Sci USA, 2004, 101(4): 1045-1050. 被引量:1

同被引文献27

  • 1Sawzdargo M, George SR, Nguyen T, et al. A cluster of four novel human G protein-coupled receptor genes occurring in close prox- inity to CD22 gene on chromosome 19q13. 1 [ J ]. Biochem Biophys Res Commun, 1997,239:543-547. 被引量:1
  • 2Basu A, Kudva Y C, Basu R. GPR40 Modulators : New kid on the block[ J ]. Diabetes Care ,2013,36 : 185-187. 被引量:1
  • 3Tetsumori Yamashima. Dual effects of the non-esterified fatty acid receptor ' GPR40' for human health[ J]. 2015,48:40-50. 被引量:1
  • 4Stefand D P, Itamar R. Introduction to the 4th world congress on Controversies to consensus in Diabetes, O-besity and Hypertension (CODHy) [ J ]. Diabet Care,2013,36 ( Suppl 2) : S111 -S112. 被引量:1
  • 5Harada Shinichi, Huruna Yuka, Aizawa Fuka, et al. Involvement of GPR40, a long-Chain free fatty acid receptor in the production of central post-stroke pain after global cerebral ischemia [ J ]. Europ J Pharmac,2014 , 744 : 115-123. 被引量:1
  • 6Nakamoto Kazuo, Aizawa Fuka, Nishinaka Takashi, et al. Regula-tion of Prohormone. Convertase 2 protein expression via GPR40/ FFA1 in the hypothalamus [ J ]. Europ J Pharmac, 2015,762 : 459-463. 被引量:1
  • 7Abaraviciene S M, Muhammed S J, Amisten S, et al. GPR40 pro- tein levels are crucial to the regulation of stimulated hormone secretion in pancreatic islets. Lessons from spontaneous obesity- prone and non-obese type 2 diabetes in rats [ J]. Molecular and Cellular Endocrinology,2013,381 (1-2) : 150-159. 被引量:1
  • 8Lu ZY, Li YC, Jin JF, et al. GPR40/FFA1 and neutral sphingo- myelinase are involved in palmitate-boosted inflammatory response of microvascular endothelial cells to LPS [ J ]. Atherosclerosis, 2015,240( 1 ) :163-173. 被引量:1
  • 9Kristinsson H, Bergsten P, Sargsyan ES. Free fatty acid receptor1 (FFA1 R/GPR40)signaling affect insulin secretion by enhancing mitochondrial respiration during palmitate exposure [ J ]. Biochim et Biophy Acta-Molec Cell Res,2015,1853 (12) :3248-3257. 被引量:1
  • 10Kruska N, Reiser G. Phytanic acid and pristanic acid, branched- chain fatty acids associated with Refusm diease and other inheri- ted peroxisomal disorders, mediate intracellular Ca2 + signaling through activation of free fatty acid receptor GPR40 [ J ]. Neurobiol Diea,2011 43(2) :465-472. 被引量:1

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