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G蛋白偶联受体119激动剂的研究进展 被引量：4

Research progress of G-protein coupled receptor 119 agonists
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摘要 G蛋白偶联受体119(GPR119)是近年来发现的治疗糖尿病药物的重要靶标。该受体激动后,既能升高血浆中GLP-1水平又能增加胰岛素的分泌,近年来受到世界多个制药公司的重视,开发了多个GPR119激动剂,部分已经进入临床研究。本文对GPR119激动剂近年来的研究进展做一综述。 G-protein-coupled receptor 119 （GPR119） has emerged as one of the most exciting targets for the treatment of type 2 diabetes. GPR119 agonists mediate a unique nutrientependent dual elevation of both insulin and glucagon like peptide 1/glucose-dependant insulinotropic peptide levels in vivo. Many pharmaceutical companies have focused on this target, several GPR119 agonists have been reported, and some of them entered clinical trials. In this article, the recent research progress of GPRll9 agonists is reviewed.
作者 蒋坤 江程 王举波 宋丽君 李志裕
机构地区 江苏省淮安市第四人民医院 中国药科大学药物化学教研室
出处 《中国新药杂志》 CAS CSCD 北大核心 2012年第20期2388-2393,共6页 Chinese Journal of New Drugs
关键词 糖尿病 GPR119激动剂 高血糖 G蛋白偶联受体 diabetes GPR119 agonists hyperglycemia G-protein-coupled receptor
分类号 R977 [医药卫生—药品]
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参考文献34

  • 1UK Prospective Diabetes Study (UKPDS) Group. Effect of inten- sive blood-glucose control with metformin on complications in o- verweight patients with type 2 diabetes ( UKPDS 34) [ J ]. Lan- cet, 1998, 352(9131). 854-865.
  • 2徐斯盛,张惠斌,周金培,黄建军.新型抗糖尿病药物的研究进展[J].中国药科大学学报,2011,42(2):97-106. 被引量：34
  • 3曹国颖,李晓翠,赵楠,刘茜,胡欣.二肽基肽酶Ⅳ抑制剂在治疗2型糖尿病的临床研究进展[J].中国新药杂志,2011,20(6):497-502. 被引量：12
  • 4LOVSHIN JA, DRUCKER DJ. Incretin-based therapies for type 2 diabetes mellitus [ J]. Nat Rev Endocrinol, 2009, 5 (5) . 262 - 269.
  • 5JONES RM, LEONARD JN, BUZARD DJ, et al. GPR119 ago- nists for the treatment of type 2 diabetes [ J ]. Expert Opin Ther Pat, 2009, 19(10). 1339-1359.
  • 6SHAH U. GPR119 agonists. a promising new approach for the treatment of type 2 diabetes and related metabolic disorders [ J ]. Curr Opin Drug Discov Devel, 2009, 12(4) . 519 -532.
  • 7FREDRIKSSON R, HOGLUND PJ, GLORIAM DE, et al. Seven evolutionarily conserved human rhodopsin G protein-coupled re- ceptors lacking close relatives [ J ]. FEBS Lett, 2003, 554 ( 3 ) .381 -388.
  • 8COSTANZI S, NEUMANN S, GERSHENGORN MC. Seven transmembranespanning receptors for free fatty acids as therapeu- tic targets for diabetes mellitus. pharmacological, phylogenetic, and drug discovery aspects[ J]. J Biol Chem, 2008, 283 (24) . 16269 - 16273.
  • 9BROWN AJ. Novel cannabinoid receptors[J]. Br J Pharmacol, 2007, 152(5) . 567 -575.
  • 10SOGA T, OHISHI T, MATSUI T, et al. Lysophosphatidylcholine enhances glucose-dependent insulin secretion via an orphan G- protein-coupled receptor [ J ]. Biochem Biophys Res Commun, 2005, 326(4). 744-751.

二级参考文献86

  • 1HANNE B. RASMUSSEN SB, FINN C. Wiberg crystal structure of human dipeptidyl peptidase IV/CD26 in complex with a substrate analog[ J]. Nat Struct Biol, 2003, 10 (1) : 19 -25.
  • 2PEI ZH, LI XF, THOMAS W VON GELDERN. Discovery of (( 4R, 5S )-5-Amino-4-( 2, 4, 5-trifluorophenyl ) cyclohex-1- enyl) -( 3-(trifluoromethyl) -5,6-dihydro-] 1,2,4 ] triazolo [ 4,3- a ] pyrazin-7 ( 8 H ) -yl) methanone ( ABT-341 ) , a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes [ J]. J Med Chem, 2006, 49 : 6439 - 6442.
  • 3DUFFY NA, GREEN BD, IRWIN N, et al. Effects of antidiabetic drugs on dipeptidyl peptidase IV activity: nateglinide is an inhibitor of DPP IV and augments the antidiabetic activity of glucagon-like peptide-1 [ J]. Eur J Pharmacol,2007, 568 ( 1 - 3 ) : 278 - 286.
  • 4HERMAN GA, STEVENS C, VAN DYCK K, et al: Pharmacokinetics and pharmacodynamics of sitagliptin, an inhibitor of dipeptidyl peptidase IV, in healthy subjects: results from two randomized, double-bllnd, placebo-controlled studies with single oral doses[J]. Clin Pharmacol Ther, 2005, 78(6) : 675 -688.
  • 5BERGMAN AJ, STEVENS C, ZHOU Y, et al. Pharmacokinetic and pharmacodynamic properties of multiple oral doses of sitagliptin, a dipeptidyl peptidase-IV inhibitor: a doubleblind, randomized, placebocontrolled study in healthy male volunteers [ J ]. Clin Ther, 2006, 28(1): 55 -72.
  • 6SUNKARA G, SABO R, WANG Y, et al. Dose proportionality and the effect of food on vildagliptin, a novel dipeptidyl peptidase IV inhibitor, in healthy volunteers[ J]. J Clin Pharmacol,2007, 47(9) : 1152 -1158.
  • 7HE YL, SABO R, CAMPESTRINI J, et al. The influence of hepatic impairment on the pharmacokinetics of the dipeptidyl peptidase IV (DPP-4) inhibitor vildagliptin [ Jl. Eur J Clin Pharmacol, 2007, 63(7) : 677 -686.
  • 8MARI A, SALLAS WM, HE YL, et al. Vildagliptin, a dipeptidyl peptidase-IV inhibitor, improves model-assessed beta-cell function in patients with type 2 diabetes [ J ]. J Clin Endocrinol Metab, 2005, 90(8): 4888-4894.
  • 9ROSENSTOCK J, FOLEY JE, RENDELL M, et al. Effects of the dipeptidyl peptidase-IV inhibitor vildagliptin on incretin hormones, islet function, and postprandial glycemia in subjects with impaired glucose tolerance [ J ]. Diabetes Care, 2008,31 ( 1 ) : 30 -35.
  • 10GALLWITZ B. Saxagliptin, a dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes [ J ]. lDrugs,2008,11 ( 12 ) : 906 - 917.

共引文献43

同被引文献35

  • 1HUSSAIN A, CLAUSSEN B, RAMACHANDRAN A. et al. Prevention of type 2 diabetes : A review [ J ]. Diabetes Res Clin Prac,2007,76930 (3) :317-326.
  • 2LINNEBJER G H, KOTHARE P A,PARK S, et al. Effect of renal impairment on the pharmacokinetics of exenatide [ J]. Br J Clin Pharmacol,2007,64(3) :317-327.
  • 3ROUBICEK T, MRA Z M, BARTLOVA M, et al. The influ- ence of 6-months treatment with exenatide on type 2 diabetes mellitus compensation , anthropometric and biochemical parameters [ J]. Vnitr Lek, 2010,56 ( 1 ) : 15- 20.
  • 4VILSBOLL T. Liraglutide:a once-daily GLP-1 analogue for the treatment of type 2 diabetes mellitus [ J ]. Expert Opin Investig Drugs,2007,16 (2) :231-237.
  • 5SOGA T, OHISHI T, MATSUI T, et al. Lysophosphatidylcholine enhances glucose-dependent insulin secretion via an orphan G- protein-coupled receptor [ J ]. Biochem Biophys Res Commun, 2005, 326(4) : 744-751.
  • 6CHU Z L, CARROLL C, ALFONSO J, et al. A role for intesti- nal endocrine cell-expressed g protein-coupled receptor 119 in glycemic control by enhancing glucagon-like Peptide-1 and glu- cose-dependent insulinotropic Peptide release [ J ]. Endocrinolo- gy. 2008. 149(5): 2038-2047.
  • 7SEEWOODHARY J, THORNTON J, BAIN S C. Experimental agents in type 2 diabetes: The next 20 years[J]. West Lond Med J, 2010, 2(3) : 29-36.
  • 8BROWN A J. Novel cannabinoid receptors [ J ]. Br J Pharma- col, 2007, 152(5): 567-575.
  • 9MADIRAJU S R M; POITOUT V. G protein-coupled receptors and insulin secretion: 119 and counting [ J ]. Endocrinology, 2007, 148(6) : 2598-2600.
  • 10LAUFFER L M, IAKOUBOY R, BRUBAKER P L GPR119 is essential for oleoylethanolamide -induced glucagon-like peptide-1 secretion from the intestinal enteroendocrine L-cell [ J ]. Diabe- tes, 2009, 58(5) : 1058-1066.

引证文献4

二级引证文献14

中国新药杂志
2012年 第20期

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