期刊文献+

Xa因子抑制剂的研究进展 被引量:6

Recent advances in the development of factor Xa
原文传递
导出
摘要 Xa因子是一个维生素K依赖的丝氨酸蛋白酶,它占据了凝血瀑布反应中的中心位置,可以由内源性和外源性凝血途径激活,其位置特殊性决定了其作用的重要性。利伐沙班等Xa因子抑制剂作为未来重要的口服抗血栓药物已上市,相关的其他方面的药理作用也成为研究热点。文中对Xa因子的结构、作用模式及不同结构抑制剂的最新研究进展做一综述。 Factor Xa (fXa) is a Vk dependent serine protease playing a crucial role in the blood coagulation cascade. It occupies the central position in the coagulation cascade as the convergence point between intrinsic and extrinsic pathways, which decides its significance in role. Rivaroxaban and several other fXa inhibitors have been approved for antithrombus treatment. Related pharmacological studies also become hotspots. In this review, we will illustrate the structure of factor Xa, the action mode between the inhibitors and fXa, and the recent research advances of fXa inhibitors with different structures.
出处 《中国新药杂志》 CAS CSCD 北大核心 2012年第20期2380-2387,共8页 Chinese Journal of New Drugs
基金 国家自然科学基金(30973638) 江苏省产学研联合创新资金-前瞻性联合研究项目(BY2011158) 先声药业研究生创新基金项目(YCH10S003XS)
关键词 XA因子 构效关系 抑制剂 抗血栓 研究进展 factor Xa structure-activity relationship inhibitors antithrombus recent advances
  • 相关文献

参考文献24

  • 1MELNIKOVA I. The anticoagulants market [ J]. Nat Rev Drug Discov, 2009, 8(5) .353 -354.
  • 2GALANIS T, THOMSON L, PALLADINO M, et al. New oral anticoagulants[ J ]. J Thromb Thrombolysis, 2011, 31 ( 3 ) . 310 - 320.
  • 3ANSELL J. Factor Xa or thrornbin. is factor Xa a better target? [ J]. J Thromb Haemost, 2007, 5 ( Suppl 1 ) . S60 - S64.
  • 4KRUPICZOJC MA, SCOTTON CJ, CHAMBERS RC. Coagula- tion signalling following tissue injury. focus on the role of factor Xa[J]. lnt J Biochem Cell Biol, 2008, 40 (6 - 7) . 1228 - 1237.
  • 5BORENSZTAJN K, PEPPELENBOSCH MP, SPEK CA. Factor Xa. at the crossroads between coagulation and signaling in physi- ology and disease [ J ]. Trends Mol Med, 2008,14 ( 10 ) . 429 - 440.
  • 6LEE YK, PLAYER MR. Developments in factor X a inhibitors for the treatment of thromboembolic disorders[ J]. Med Res Rev, 2011, 31(2) .202 -283.
  • 7VAN GOGH INVESTIGATORS, BULLER HR, COHEN AT, et al. Extended prophylaxis of venous thromboembolism with id- raparinux[J]. NEnglJMed, 2007, 357(11) .1105-1112.
  • 8PATY I, TRELLU M, DESTORS JM, et al. Reversibility of the anti-FXa activity of idrabiotaparinux (biotinylated idraparinux) by intravenous avidin infusion[J]. J Thromb Haemost, 2010, 8 (4) .722 -729.
  • 9Sanofi-aventis Press Release. Sanofi-aventis provides an R&D Pipeline update [ N]. 2009 - 10 -21. http.//en, san0fi-avent- is. com/binaries/20091221_rdupdate en tcm28-26977, pdf.
  • 10KOH CY, KINI RM. Molecular di'~ersity of anticoagulants from haematophagous animals [ J ]. Thromb Haemost, 2009, 102 (3) . 437 - 453.

二级参考文献25

  • 1Beaglehole R, Bonita R. Global public health: a scorecard [ J ]. Lancet,2008,372(9 654) :1 988 -1 996.
  • 2Mathers CD, Loncar D. Projections of global mortality and burden of disease from 2002 to 2030 [ J ]. PLoS Med, 2006, 3 (11) : e442.
  • 3Saiah E,Soares C. Small molecule coagulation cascade inhibitors in the clinic[J]. Curr Top Med Chem,2005,5(16) :1 677 - 1 695.
  • 4Abbenante G, Fairlie DP. Protease inhibitors in the clinic [ J ]. Med Chem,2005,1 ( 1 ) :71 - 104.
  • 5Borensztajn K, Peppelenbosch MP, Spek CA. Factor Xa: at the crossroads between coagulation and signaling in physiology and disease[ J ]. Trends Mol Meal,2008,14(10) :429 -440.
  • 6Brandstetter H, Kuhne A, Bode W,et al. X-ray structure of active site-inhibited clotting factor Xa [ J ]. J Biol Chem, 1996, 271 (47) :29 988 -29 992.
  • 7Daure EW, Fujikawa K,Kisiel W. The coagulation cascude:initiation, maintenance and regulation [ J ]. Biochemistry, 1991,30 (43) :10 363 -10 370.
  • 8Ansell J. Factor Xa or thrombin :is factor Xa a better target [ J ] ?J Thromb Haemost,2007,5( Suppl 1 ) :60 -64.
  • 9Roehrig S, Straub A, Pohlmann J, et al. Discovery of the novel antithrombotic agent 5-ehloro-N- ( { ( 5 S ) -2 -oxo-3- [ 4- ( 3-oxomor- pholin-4-yl ) phenyl ] -1,3-oxazolidin-5-yl } methyl ) thiophene-2- carboxamide( BAY 59-7939 ) : an oral, direct factor Xa inhibitor [ J]. J Med Chem,2005,48(19) :5 900 -5 908.
  • 10Lam PY, Clark CG, Li R, et al. Structure-based design of novel guanidine/benzamidine mimics: potent and orally bioavailable factor Xa inhibitors as novel anticoagulants [J]. J Med Chem, 2003,46(21 ) :4 405 -4 418.

共引文献6

同被引文献67

  • 1吴丹,王静,王艳,刘龙.噁唑烷酮类化合物的合成及其凝血因子Ⅹa抑制活性研究[J].中国药物化学杂志,2019,29(6):426-432. 被引量:1
  • 2XinPing Luo,KeLi Wang,Hao Jiang,Jia Sun,JuanJuan Xu,QingLiang Zhu,ZhaoGuo Li.Advances in research of land surface evapotranspiration at home and abroad[J].Research in Cold and Arid Regions,2010,2(2):104-111. 被引量:1
  • 3Jean-Noel,Fiessinger,MD,Menno,V.,Huisman,,MD,Bruce,L.,Davidson,,MD,王莉华(译),诸骏仁(校).Ximelagatran与低分子肝素加华法令治疗深静脉血栓的比较 随机试验[J].美国医学会杂志(中文版),2005,24(6):370-370. 被引量:2
  • 4黄园园,戴秋云.抗凝血多肽及类肽研究进展[J].中国生化药物杂志,2007,28(5):349-352. 被引量:12
  • 5Bondarenko M,Curti C,Montana M,et al.Efficacy andtoxicity of factor Xa inhibitors [J].J Pharm Pharm Sci,2013,16(1): 74-88.
  • 6Genovesi S,Rossi E,Gallieni M,et al.Warfarin use,mortality,bleeding and stroke in haemodialysis patientswith atrial fibrillation [J].Nephrol Dial Transplant,2014,28(8): 1-8.
  • 7Ranganathan R L,Venkatesh P.Atrial fibrillation andstroke prevention: is warfarin still an option?—No.[J].JNeural Transm,2013,120(10): 1453-1456.
  • 8Lee Y K,Player M R.Developments in factor Xainhibitors for the treatment of thromboembolic disorders[J].Med Res Rev,2011,31(2): 202-283.
  • 9Zhang P,Huang W,Wang L,et al.Discovery ofbetrixaban (PRT054021),N-(5-chloropyridin-2-yl)-2-(4-N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide,a highly potent,selective,and orally efficaciousfactor Xa inhibitor [J].Bioorg Med Chem Lett,2009,19(8): 2179-2185.
  • 10Morganroth J,Gretler D D,Hollenbach S J,et al.Absenceof QTc prolongation with betrixaban: a randomized,double-blind,placebo- and positive-controlled thorough ECGstudy [J].Expert Opin Pharmacother,2013,14(1): 5-13.

引证文献6

二级引证文献14

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