期刊文献+

果糖-1,6-二磷酸酶AMP变构抑制剂的研究进展 被引量:3

Recent advance in the discovery of allosteric inhibitors binding to the AMP site of fructose-1,6-bisphosphatase
原文传递
导出
摘要 果糖-1,6-二磷酸酶(fructose-1,6-bisphosphatase,FBPase)是肝葡萄糖异生路径中的一个限速酶,催化果糖-1,6-二磷酸水解为果糖-6-磷酸。抑制FBPase的活性,可减少内源性葡萄糖的生成,降低血糖水平,FBPase抑制剂是潜在的新型治疗Ⅱ型糖尿病的药物。本文综述了近年来FBPase一磷酸腺苷(adenosine monophosphate,AMP)变构抑制剂研究的最新进展。 Fructose-1,6-bisphosphatase(FBPase),a rate-limiting enzyme involved in the pathway of gluconeogenesis,can catalyze the hydrolysis of fructose-1,6-bisphosphate to fructose-6-phosphate.Upon inhibiting the activity of FBPase,the production of endogenous glucose can be decreased and the level of blood glucose lowered.Therefore,inhibitors of FBPase are expected to be novel potential therapeutics for the treatment of type II diabetes.Recent research efforts were reviewed in the field of developing allosteric inhibitors interacting with the AMP binding site of FBPase.
出处 《药学学报》 CAS CSCD 北大核心 2011年第11期1291-1300,共10页 Acta Pharmaceutica Sinica
关键词 果糖-1 6-二磷酸酶 FBPase抑制剂 糖尿病 fructose 1 6-bisphosphatase FBPase inhibitor diabetes
  • 相关文献

参考文献26

  • 1Yang WY, Lu JM, Weng JP, et al. Prevalence of diabetes among men and women in China [J]. New Engl J Med, 2010, 362: 1090-1101.
  • 2Ke HM, Liang JY, Zhang YP, et al. Conformational transition of fructose-I, 6-bisphosphatase: structure comparison between the AMP complex (T form) and the fructose 6-phosphate complex (R form) [J]. Biochemistry, 1991,30: 4412-4420.
  • 3Bruce EM, Allen BR, Gene FT, et al. Stereoselective synthesis and biological activity of betaand alpha-D-arabinose 1, 5diphosphate: analogs of a potent metabolic regulator [J]. J Am Chem Soc, 1984, 106: 7851-7853.
  • 4Pilkis S J, McGrane MM, Kountz PD, et al. The effect of arabinose I, 5-bisphosphate on rat hepatic 6-phosphofructo-1kinase and fructose-l, 6-bisphosphatase [J]. Biochem Biophys Res Commun, 1986, 138: 159-166.
  • 5Wright SW, Hageman DL, McClure LD, et al. Allosteric inhibition of fructose-l, 6-bisphosphatase by anilinoquinazolines [J]. Bioorg Med Chem Lett, 2001, 11 : 17-21.
  • 6Wright SW, Hageman DL, McClure LD, et al. Anilinoquinazoline inhibitors of fructose 1,6-bisphosphatase bind at a novel allosteric site: synthesis, in vitro characterization, and X-ray crystallography [J]. J Med Chem, 2002, 45: 3865-3877.
  • 7Rosini M, Mancini F, Tarozzi A, et al. Design, synthesis, and biological evaluation of substituted 2, 3-dihydro-lH-cyclopenta [b] quinolin-9-ylamine related compounds as fructose-I, 6bisphosphatase inhibitors [J]. Bioorg Med Chem, 2006, 14:7846-7853.
  • 8Gidh-Jain M, Zhang YP, van Poelje PD, et al. The allostefic site of human liver fructose-l, 6-bisphosphatase. Analysis of six AMP site mutants based on the crystal structure [J]. J Biol Chem, 1994, 269: 27732-27738.
  • 9Wright SW, Carlo AA, Danley DE, et al. 3-(2-Carboxy-ethyl)4, 6-dichloro-lH-indole-2-carboxylic acid: an allosteric inhibitor of fructose-l, 6-bisphosphatase at the AMP site [J]. Bioorg Med Chem Lett, 2003, 13: 2055-2058.
  • 10yon Geldern TW, Lai CQ, Gum RJ, et al. Benzoxazole benzenesulfonamides are novel allosteric inhibitors of fructose1, 6-bisplaosphatase with a distinct binding mode [J]. Bioorg Med Chem Let-t, 2006, 16: 1811-1815.

同被引文献11

  • 1Lin H, Decuypere E,Buyse J. Oxidative stress induced by corticosterone administration in broiler chickens (Gallus gallus domesticus) : 1. Chronic exposure[J]. Comp Biochem Physiol B Biochem Mol Biol, 2004, 139 (4) : 737-744.
  • 2Agrawal A,Jaggi A S,Singh N. Pharmacological in- vestigations on adaptation in rats subjected to cold water immersion stress[J]. Physiology ~ Behavior, 2011,103 (3-4) : 321-329.
  • 3Nagamatsu S, Nakamichi Y, Yamamura C, et al. Decreased expression of t-SNARE, syntaxin 1, and SNAP-25 in pancreatic beta-cells is involved in im- paired insulin secretion from diabetic GK rat islets: Restoration of decreased t-SNARE proteins improves impaired insulin secretion[J]. Diabetes, 1999, 48(12) .- 2367 2373.
  • 4Bell G I,Polonsky K S. Diabetes mellitus and geneti- cally programmed defects in beta-cell function[J]. Nature, 2002,414(6865) : 788-791.
  • 5Matschinsky F M, Glaser B, Magnuson M A. Pancre- atic beta-cell glucokinase: Closing the gap between theoretical concepts and experimental realities [J]. Diabetes, 1998,47 (3) . 307-315.
  • 6Hangalapura B N. Cold stress equally enhances in vivo pro-inflammatory cytokine gene expression in chicken lines divergently selected for antibody respon- ses[J]. Developmental ~ Comparative Immunology, 2006,30(5) :503 511.
  • 7李丽娟,王安,芦燕.冷应激对肉仔鸡生长性能、免疫及抗氧化功能的影响[J].中国饲料,2009(17):42-43. 被引量:9
  • 8屠云洁,耿照玉,陈国宏,苏一军.动物冷应激反应中多种基因调控机制的研究[J].中国畜牧兽医,2010,37(1):84-87. 被引量:4
  • 9马文涛,杨来启,林玉梅,王晓峰,刘光雄,吴兴曲,张红宾,原亚文,王蓉蓉.应激对大鼠血清皮质醇及白细胞介素2、6、8水平的影响[J].中国心理卫生杂志,2002,16(1):14-15. 被引量:39
  • 10罗海吉,吉雁鸿,张云山,卢晓翠.高温应激下补充L-精氨酸对小鼠免疫功能的影响[J].氨基酸和生物资源,2002,24(1):35-38. 被引量:14

引证文献3

二级引证文献6

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部