期刊文献+

白三烯A4水解酶及其抑制药研究进展 被引量:3

下载PDF
导出
摘要 白三烯是从花生四烯酸代谢产物中分离得到的具有共轭三烯结构的二十碳不饱和酸,白三烯A4水解酶是水解白三烯A4产生白三烯B4的关键酶,具有环氧化物水解酶及氨肽酶双重活性。白三烯B4是许多急性和慢性炎症的重要化学递质,广泛参与诸多炎症性疾病的发生。除了在炎症发生发展过程中扮演重要角色,近期的研究表明,白三烯A4水解酶与多种恶性肿瘤的发生息息相关。因此,新型白三烯A4水解酶抑制药的研发工作对研制新型抗炎抗肿瘤药物具有十分重要的意义。该文就白三烯A4水解酶及其抑制药的研究进展作一综述。
出处 《医药导报》 CAS 2015年第2期225-227,共3页 Herald of Medicine
基金 天津市应用基础及前沿技术研究计划自然科学基金一般项目(12JCYBJC31600)
  • 相关文献

参考文献17

  • 1刘莹,陈政,尚尔昌,杨坤,位灯国,周璐,蒋小蕗,贺冲,来鲁华.花生四烯酸代谢网络研究:从关键酶的单靶标抑制剂到多靶标抑制剂[J].药学学报,2009,44(3):231-241. 被引量:26
  • 2李凤林.白三烯的研究现状.哈尔滨医科大学学报,1984,18(1):69-76.
  • 3THUNNISSEN M M,NORDLUND P,HAEGGSTROM J Z.Crystal structure of human leukotriene A (4) hydrolase,abifunctional enzyme in inflammation [ J ]. Nat Struct Biol,2001,8(2) :131-135.
  • 4PORAS H,DUQUESNOY S,FOURNIE-ZALUSKI M C,etal. A sensitive fluorigenic substrate for selective in vitro andin vivo assay of leukotriene A4 hydrolase activity[ J]. AnalBiochem,2013,441 (2) :27376-27382.
  • 5JIANG X,ZHOU L,WU Y,et al. Modulating the substratespecificity of LTA4 H aminopeptidase by using chemicalcompounds and small-molecule-guided mutagenesis [ J ].Chem Bio Chem,2010,11 (8) :1120-1128.
  • 6CHEN X, WANG S, WU N,et al. Leukotriene A4hydrolaseas a target for cancer prevention and therapy [ J ]. CurrCancer Drug Targets,2004,4(3) :267-283.
  • 7SANDANAYAKA V,MAMAT B,MISHRA R K,et al. Dis-covery of 4-[ ( 25 ) -2- j [ 4-( 4-Chlorophenoxy ) phenoxy ]methyl} -1-pyrrolidinyl ] -butanoic acid ( DG-051 ) as anovel leukotriene A4 hydrolase inhibitor of leukotriene B4biosynthesis[ J] . J Med Chem,2010,53 (2) :573-585.
  • 8JIANG X,ZH0U L,WEI D,et al. Activation and inhibitionof leukotriene A4 hydrolase aminopeptidase activity bydiphenyl ether and derivatives[ J]. Bioorg Med Chem Lett,2008,18(24) :6549-6552.
  • 9ENOMOTO H, MORIKAWA Y, MIYAKE Y, et al. Synthesisand biological evaluation of /V-mercaptoacylcysteinederivatives as leukotriene A4 hydrolase inhibitors [ J ].Bioorg Med Chem Lett,2009 ,19(2) :442-446.
  • 10WEI D, JIANG X, ZHOU L, et al. Discovery of multi targetinhibitors by combining molecular docking with commonpharmacophore matching[ J]. J Med Chem,2008,51 (24):7882-7888.

二级参考文献64

  • 1Miller DK, Gillard JW, Vickers P J, et al. Identification and isolation of a membrane-protein necessary for leukotriene production [J]. Nature, 1990, 343: 278-281.
  • 2Tsuji F, Oki K, Fujisawa K, et al. Involvement of leukotriene B4 in arthritis models [J]. Life Sci, 1998, 64: 151-156.
  • 3Penning TD. Inhibitors of leukotriene A4 (LTA4) hydrolase as potential anti-inflammatory agents [J]. Curr Pharm Des, 2001, 7: 163-179.
  • 4Penning TD, Chandrakumar NS, Desai BN, et al. Synthesis of imidazopyridines and purines as potent inhibitors of leukotriene A4 hydrolase [J]. Bioorg Med Chem Lett, 2003, 13: 1137-1139.
  • 5Grice CA, Tays KL, Savall BM, et al. Identification of a potent, selective, and orally active leukotriene A4 hydrolase inhibitor with anti-inflammatory activity [J]. J Med Chem, 2008, 51: 4150-4169.
  • 6Ye B, Bauman J, Chen M, et al. Synthesis of N-alkyl glycine amides as potent inhibitors of leukotriene A4 hydrolase [J]. Bioorg Med Chem Lett, 2008, 18: 3891-3894.
  • 7Haeggstrom JZ. Leukotriene A4 hydrolase/aminopeptidase, the gatekeeper of chemotactic leukotriene B4 biosynthesis [J]. J Biol Chem, 2004, 279: 50639-50642.
  • 8Thunnissen MM, Andersson B, Samuelsson B, et al. Crystal structures of leukotriene A4 hydrolase in complex with captopril and two competitive tight-binding inhibitors [J]. FASEB J, 2002, 16: 1648-1650.
  • 9Schrattenholz A, Soskic V. What does systems biology mean for drug development? [J]. Curr Med Chem, 2008, 15: 1520- 1528.
  • 10Yang K, Bai HJ, Ouyang Q, et al. Finding multiple target optimal intervention in disease-related molecular network [J]. Mol Syst Biol, 2008, 4: 228.

共引文献25

同被引文献17

引证文献3

二级引证文献24

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