메뉴 건너뛰기




Volumn 11, Issue 4, 2008, Pages 480-486

TAFIa inhibitors in the treatment of thrombosis

Author keywords

Carboxypeptidase; Carboxypeptidase U; Inhibitor; TAFIa; Thrombosis; Zinc metalloprotease

Indexed keywords

2 AMINOPYRIDINE DERIVATIVE; 3 (2 GUANIDINOETHYLTHIO) 2 (MERCAPTOMETHYL)PROPIONIC ACID; ACTIVATED THROMBIN ACTIVATABLE FIBRINOLYSIS INHIBITOR; ALTEPLASE; AZD 9684; BX 528; CAPTOPRIL; DIPEPTIDYL CARBOXYPEPTIDASE; EF 6265; ENALAPRIL; FIBRIN; IMIDAZOLE DERIVATIVE; PHOSPHINIC ACID DERIVATIVE; SAR 104772; SQ 24798; THROMBIN ACTIVATABLE FIBRINOLYSIS INHIBITOR; UK 396082; ZINC;

EID: 46749103227     PISSN: 13676733     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review
Times cited : (22)

References (43)
  • 1
    • 24944454291 scopus 로고    scopus 로고
    • Carboxypeptidase U (TAFIa): A metallocarboxypeptidase with a distinct role in hemostasis and a possible risk factor for thrombotic disease
    • Leurs J, Hendriks D: Carboxypeptidase U (TAFIa): A metallocarboxypeptidase with a distinct role in hemostasis and a possible risk factor for thrombotic disease. Thromb Haemost (2005) 94(3):471-487.
    • (2005) Thromb Haemost , vol.94 , Issue.3 , pp. 471-487
    • Leurs, J.1    Hendriks, D.2
  • 2
    • 28444457265 scopus 로고    scopus 로고
    • The discovery of TAFI
    • •• Provides a definitive review of the research into TAFI by one of the discoverers of the zymogen
    • Nesheim M, Bajzar L: The discovery of TAFI. J Thromb Haemost (2005) 3(10):2139-2146. •• Provides a definitive review of the research into TAFI by one of the discoverers of the zymogen.
    • (2005) J Thromb Haemost , vol.3 , Issue.10 , pp. 2139-2146
    • Nesheim, M.1    Bajzar, L.2
  • 3
    • 0017111539 scopus 로고
    • Homologous inhibitors from potato tubers of serine endopeptidases and metallocarboxypeptidases
    • Hass CM, Venkatakrishnan R, Ryan CA: Homologous inhibitors from potato tubers of serine endopeptidases and metallocarboxypeptidases. Proc Natl Acad Sci USA (1976) 73(6):1941-1944.
    • (1976) Proc Natl Acad Sci USA , vol.73 , Issue.6 , pp. 1941-1944
    • Hass, C.M.1    Venkatakrishnan, R.2    Ryan, C.A.3
  • 4
    • 0029793068 scopus 로고    scopus 로고
    • The profibrinolytic effect of activated protein C in clots formed from plasma is TAFI-dependent
    • Bajzar L, Nesheim ME, Tracy PB: The profibrinolytic effect of activated protein C in clots formed from plasma is TAFI-dependent. Blood (1996) 88(6):2093-2100.
    • (1996) Blood , vol.88 , Issue.6 , pp. 2093-2100
    • Bajzar, L.1    Nesheim, M.E.2    Tracy, P.B.3
  • 5
    • 0017578611 scopus 로고
    • Design of specific inhibitors of angiotensin-converting enzyme: New class of orally active antihypertensive agents
    • Ondetti MA, Rubin B, Cushman DW: Design of specific inhibitors of angiotensin-converting enzyme: New class of orally active antihypertensive agents. Science (1977) 196(4288):441-444.
    • (1977) Science , vol.196 , Issue.4288 , pp. 441-444
    • Ondetti, M.A.1    Rubin, B.2    Cushman, D.W.3
  • 6
    • 0001518155 scopus 로고    scopus 로고
    • A new type of carboxypeptidase A inhibitors designed using an imidazole as a zinc coordinating ligand
    • Provides an early and rare example of the use of an imidazole as a ligand for coordinating zinc in a carboxypeptidase inhibitor, •
    • Lee KJ, Joo KC, Kim E-J, Lee M, Kim DH: A new type of carboxypeptidase A inhibitors designed using an imidazole as a zinc coordinating ligand. Bioorg Med Chem (1997) 5(10):1989-1998. • Provides an early and rare example of the use of an imidazole as a ligand for coordinating zinc in a carboxypeptidase inhibitor.
    • (1997) Bioorg Med Chem , vol.5 , Issue.10 , pp. 1989-1998
    • Lee, K.J.1    Joo, K.C.2    Kim, E.-J.3    Lee, M.4    Kim, D.H.5
  • 9
    • 37849034911 scopus 로고    scopus 로고
    • Bunnage ME, Blagg J, Steele J, Owen DR, Allerton C, McElroy AB, Miller D, Ringer T, Butcher K, Beaumont K, Evans K et al: Discovery of potent & selective inhibitors of activated thrombin-activatable fibrinolysis inhibitor for the treatment of thrombosis. J Med Chem (2007) 50(24):6095-6103. •• Provides a full description of the program to convert a non-selective thiol lead into a selective, imidazole-based development candidate. This is a rare example of published phase I toleration data and human pharmacokinetic data in the research area of TAFI.
    • Bunnage ME, Blagg J, Steele J, Owen DR, Allerton C, McElroy AB, Miller D, Ringer T, Butcher K, Beaumont K, Evans K et al: Discovery of potent & selective inhibitors of activated thrombin-activatable fibrinolysis inhibitor for the treatment of thrombosis. J Med Chem (2007) 50(24):6095-6103. •• Provides a full description of the program to convert a non-selective thiol lead into a selective, imidazole-based development candidate. This is a rare example of published phase I toleration data and human pharmacokinetic data in the research area of TAFI.
  • 10
    • 33846907430 scopus 로고    scopus 로고
    • Islam I, Bryant J, May K, Mohan R, Yuan S, Kent L, Morser J, Zhao L, Vergona R, White K, Adler M et al: 3-Mercaptopropionic acids as efficacious inhibitors of activated thrombin activatable fibrinolysis inhibitor (TAFIa). Bioorg Med Chem Lett (2007) 17(5):1349-1354. • Provides the only published literature on the Berlex Biosciences thiol program. The research demonstrates how carboxypeptidase N selectivity was improved, and provides some evidence for preclinical efficacy and safety.
    • Islam I, Bryant J, May K, Mohan R, Yuan S, Kent L, Morser J, Zhao L, Vergona R, White K, Adler M et al: 3-Mercaptopropionic acids as efficacious inhibitors of activated thrombin activatable fibrinolysis inhibitor (TAFIa). Bioorg Med Chem Lett (2007) 17(5):1349-1354. • Provides the only published literature on the Berlex Biosciences thiol program. The research demonstrates how carboxypeptidase N selectivity was improved, and provides some evidence for preclinical efficacy and safety.
  • 12
    • 46749083163 scopus 로고    scopus 로고
    • DailyDrugNews.com: AstraZeneca updates status of development portfolio. Prous Science Daily Essentials (2006) June 13.
    • DailyDrugNews.com: AstraZeneca updates status of development portfolio. Prous Science Daily Essentials (2006) June 13.
  • 14
    • 24944445159 scopus 로고    scopus 로고
    • Inhibition of carboxypeptidase U (TAFIa) activity improves rt-PA induced thrombolysis in a dog model of coronary artery thrombosis
    • Björkman JE, Abrahamsson TI, Nerme VK, Mattsson CJ: Inhibition of carboxypeptidase U (TAFIa) activity improves rt-PA induced thrombolysis in a dog model of coronary artery thrombosis. Thromb Res (2005) 116(6):519-524.
    • (2005) Thromb Res , vol.116 , Issue.6 , pp. 519-524
    • Björkman, J.E.1    Abrahamsson, T.I.2    Nerme, V.K.3    Mattsson, C.J.4
  • 16
    • 33846947189 scopus 로고    scopus 로고
    • Wang YX, da Cunha V, Vincelette J, Zhao L, Nagashima M, Kawai K, Yuan S, Emayan K, Islam I, Hosoya J, Sullivan ME et al: A novel inhibitor of activated thrombin activatable fibrinolysis inhibitor (TAFIa) - Part II: Enhancement of both exogenous and endogenous fibrinolysis in animal models of thrombosis. Thromb Haemost (2007) 97(1):54-61. •• Reports pharmacokinetic, efficacy and preclinical safety data for BRX-528 from Berlex Biosciences.
    • Wang YX, da Cunha V, Vincelette J, Zhao L, Nagashima M, Kawai K, Yuan S, Emayan K, Islam I, Hosoya J, Sullivan ME et al: A novel inhibitor of activated thrombin activatable fibrinolysis inhibitor (TAFIa) - Part II: Enhancement of both exogenous and endogenous fibrinolysis in animal models of thrombosis. Thromb Haemost (2007) 97(1):54-61. •• Reports pharmacokinetic, efficacy and preclinical safety data for BRX-528 from Berlex Biosciences.
  • 19
    • 11144356646 scopus 로고    scopus 로고
    • Suzuki K, Muto Y, Fushihara K, Kanemoto K, Iida H, Sato E, Kikuchi C, Matsushima T, Kato E, Nomoto M, Yoshioka S et al: Enhancement of fibrinolysis by EF-6265 [(S)-7-amino-2-[[[(R)-2- methyl-1-(3-phenylpropanoylamino)propyl]hydroxyphosphinoyl] methyl]heptanoic acid], a specific inhibitor of plasma carboxypeptidase B. J Pharmacol Exp Ther (2004) 309(2):607-615. •• Provides evidence for the renal protective properties of EF-6265, the TAFIa inhibitor that is being researched by Meiji Seika Kaisha.
    • Suzuki K, Muto Y, Fushihara K, Kanemoto K, Iida H, Sato E, Kikuchi C, Matsushima T, Kato E, Nomoto M, Yoshioka S et al: Enhancement of fibrinolysis by EF-6265 [(S)-7-amino-2-[[[(R)-2- methyl-1-(3-phenylpropanoylamino)propyl]hydroxyphosphinoyl] methyl]heptanoic acid], a specific inhibitor of plasma carboxypeptidase B. J Pharmacol Exp Ther (2004) 309(2):607-615. •• Provides evidence for the renal protective properties of EF-6265, the TAFIa inhibitor that is being researched by Meiji Seika Kaisha.
  • 21
    • 46749083991 scopus 로고    scopus 로고
    • Thrombin-activatable fibrinolysis inhibitor and deep vein thrombosis
    • Gao H, Xu Y, Xu C: Thrombin-activatable fibrinolysis inhibitor and deep vein thrombosis. Xueshuan Yu Zhixuexue (2006) 12(6):276-278.
    • (2006) Xueshuan Yu Zhixuexue , vol.12 , Issue.6 , pp. 276-278
    • Gao, H.1    Xu, Y.2    Xu, C.3
  • 22
    • 38349054795 scopus 로고    scopus 로고
    • Thrombin activatable fibrinolysis inhibitor activity, thrombin-antithrombin complex and D-dimer levels in preterm neonates with early respiratory distress syndrome
    • Gursoy T, Tekinalp G, Yurdakok M, Ozcebe O, Korkmaz A, Gurgey A: Thrombin activatable fibrinolysis inhibitor activity, thrombin-antithrombin complex and D-dimer levels in preterm neonates with early respiratory distress syndrome. Am J Hematol (2007) 83(1):50-53.
    • (2007) Am J Hematol , vol.83 , Issue.1 , pp. 50-53
    • Gursoy, T.1    Tekinalp, G.2    Yurdakok, M.3    Ozcebe, O.4    Korkmaz, A.5    Gurgey, A.6
  • 23
    • 34247891640 scopus 로고    scopus 로고
    • Thrombin activatable fibrinolysis inhibitor and its relationship to fibrinolysis and inflammation during the acute and convalescent phase of ischemic stroke
    • Rooth E, Wallen H, Antovic A, von Arbin M, Kaponides G, Wahlgren N, Blombaeck M, Antovic J: Thrombin activatable fibrinolysis inhibitor and its relationship to fibrinolysis and inflammation during the acute and convalescent phase of ischemic stroke. Blood Coagul Fibrinolysis (2007) 18(4):365-370.
    • (2007) Blood Coagul Fibrinolysis , vol.18 , Issue.4 , pp. 365-370
    • Rooth, E.1    Wallen, H.2    Antovic, A.3    von Arbin, M.4    Kaponides, G.5    Wahlgren, N.6    Blombaeck, M.7    Antovic, J.8
  • 27
    • 33749543001 scopus 로고    scopus 로고
    • Postprandial thrombin activatable fibrinolysis inhibitor and markers of endothelial dysfunction in type 2 diabetic patients
    • Rigla M, Wägner AM, Borrell M, Mateo J, Foncuberta J, de Leiva A, Ordóñez-Llanos J, Pérez A: Postprandial thrombin activatable fibrinolysis inhibitor and markers of endothelial dysfunction in type 2 diabetic patients. Metabolism (2006) 55(11):1437-1442.
    • (2006) Metabolism , vol.55 , Issue.11 , pp. 1437-1442
    • Rigla, M.1    Wägner, A.M.2    Borrell, M.3    Mateo, J.4    Foncuberta, J.5    de Leiva, A.6    Ordóñez-Llanos, J.7    Pérez, A.8
  • 28
    • 4444287314 scopus 로고    scopus 로고
    • Thrombin-activatable fibrinolysis inhibitor
    • Marx PF: Thrombin-activatable fibrinolysis inhibitor. Curr Med Chem (2004) 11(17):2335-2348.
    • (2004) Curr Med Chem , vol.11 , Issue.17 , pp. 2335-2348
    • Marx, P.F.1
  • 29
    • 33846926328 scopus 로고    scopus 로고
    • Thrombin activatable fibrinolysis inhibitor (TAFI): A role in pre-eclampsia?
    • Dusse LM, Cooper AJ, Lwaleed BA: Thrombin activatable fibrinolysis inhibitor (TAFI): A role in pre-eclampsia? Clin Chim Acta (2007) 378(1-2):1-6.
    • (2007) Clin Chim Acta , vol.378 , Issue.1-2 , pp. 1-6
    • Dusse, L.M.1    Cooper, A.J.2    Lwaleed, B.A.3
  • 30
    • 34250182769 scopus 로고    scopus 로고
    • Assessment of the role of thrombin activatable fibrinolysis inhibitor in retinal vein occlusion
    • Gumus K, Kadayifcilar S, Eldem B, Ozcebe O: Assessment of the role of thrombin activatable fibrinolysis inhibitor in retinal vein occlusion. Retina (2007) 27(5):578-583.
    • (2007) Retina , vol.27 , Issue.5 , pp. 578-583
    • Gumus, K.1    Kadayifcilar, S.2    Eldem, B.3    Ozcebe, O.4
  • 33
    • 2942755757 scopus 로고    scopus 로고
    • Thrombin activatable fibrinolysis inhibitor: Not just an inhibitor of fibrinolysis
    • Provides a full perspective on the potential for TAFIa inhibitors beyond thrombosis, ••
    • Bajzar L, Jain N, Wang P, Walker JB: Thrombin activatable fibrinolysis inhibitor: Not just an inhibitor of fibrinolysis. Crit Care Med (2004) 32(5 Suppl):S320-S324. •• Provides a full perspective on the potential for TAFIa inhibitors beyond thrombosis.
    • (2004) Crit Care Med , vol.32 , Issue.5 SUPPL.
    • Bajzar, L.1    Jain, N.2    Wang, P.3    Walker, J.B.4
  • 34
    • 46749136946 scopus 로고    scopus 로고
    • SANOFI-AVENTIS DEUTSCHLAND GMBH (Lindenschmidt A, Kallus C, Heitsch H, Grueneberg S, Szillat H): Imidazole derivatives as TAFIa inhibitors. US-20070129341 (2007).
    • SANOFI-AVENTIS DEUTSCHLAND GMBH (Lindenschmidt A, Kallus C, Heitsch H, Grueneberg S, Szillat H): Imidazole derivatives as TAFIa inhibitors. US-20070129341 (2007).
  • 35
    • 46749144694 scopus 로고    scopus 로고
    • SANOFI-AVENTIS (Wehner V, Kallus C, Heitsch H): Imidazole derivatives as inhibitors of TAFIa. WO-2007045339 (2007).
    • SANOFI-AVENTIS (Wehner V, Kallus C, Heitsch H): Imidazole derivatives as inhibitors of TAFIa. WO-2007045339 (2007).
  • 36
    • 46749132439 scopus 로고    scopus 로고
    • AVENTIS RESEARCH & TECHNOLOGIES (Kallus C, Heitsch H, Lindenschmidt A, Grueneberg S): Imidazole derivatives used as TAFIa inhibitors. WO-2005105781 (2005).
    • AVENTIS RESEARCH & TECHNOLOGIES (Kallus C, Heitsch H, Lindenschmidt A, Grueneberg S): Imidazole derivatives used as TAFIa inhibitors. WO-2005105781 (2005).
  • 37
    • 46749153154 scopus 로고    scopus 로고
    • PFIZER INC (Allerton CM, Blagg J, Bunnage ME, Steele J): Substituted imidazoles as TAFIa inhibitors. WO-02014285 (2002).
    • PFIZER INC (Allerton CM, Blagg J, Bunnage ME, Steele J): Substituted imidazoles as TAFIa inhibitors. WO-02014285 (2002).
  • 38
    • 46749099926 scopus 로고    scopus 로고
    • ASTRAZENECA AB (Linschoten M, Polla M): Potential inhibitors of carboxypeptidase U. WO-00066550 (2000).
    • ASTRAZENECA AB (Linschoten M, Polla M): Potential inhibitors of carboxypeptidase U. WO-00066550 (2000).
  • 39
    • 46749152734 scopus 로고    scopus 로고
    • Linschoten M, Polla M: Phosphinyloxy, oxime and carboxylic acid derivatives which are useful as carboxypeptidase U inhibitors. US-20060079484 (2006).
    • Linschoten M, Polla M: Phosphinyloxy, oxime and carboxylic acid derivatives which are useful as carboxypeptidase U inhibitors. US-20060079484 (2006).
  • 40
    • 46749149821 scopus 로고    scopus 로고
    • ASTRAZENECA AB (Polla M): Preparation of phosphoryl propanoic acid derivatives as inhibitors of carboxypeptidase U. WO-03027128 (2003).
    • ASTRAZENECA AB (Polla M): Preparation of phosphoryl propanoic acid derivatives as inhibitors of carboxypeptidase U. WO-03027128 (2003).
  • 41
    • 46749143452 scopus 로고    scopus 로고
    • MEIJI SEIKA KAISHA LTD (Fushihara K, Kikuchi C, Matsushima T, Kanemoto K, Satoh E, Yamamoto T, Suzuki K): Phosphonic acid derivatives having carboxypeptidase B inhibitory activity. WO-01019836 (2001).
    • MEIJI SEIKA KAISHA LTD (Fushihara K, Kikuchi C, Matsushima T, Kanemoto K, Satoh E, Yamamoto T, Suzuki K): Phosphonic acid derivatives having carboxypeptidase B inhibitory activity. WO-01019836 (2001).
  • 42
    • 46749137333 scopus 로고    scopus 로고
    • BAYER SCHERING PHARMA AG/MIE UNIVERSITY SCHOOL OF MEDICINE (Gabazza EC, Taguchi O, Fujimoto HM): TAFI inhibitors and their use to treat pulmonary fibrosis. WO-06041808 (2006).
    • BAYER SCHERING PHARMA AG/MIE UNIVERSITY SCHOOL OF MEDICINE (Gabazza EC, Taguchi O, Fujimoto HM): TAFI inhibitors and their use to treat pulmonary fibrosis. WO-06041808 (2006).
  • 43
    • 46749159034 scopus 로고    scopus 로고
    • ASTRAZENECA AB (Björquist P, Buchanan M, Campitelli M, Carroll A, Hyde E, Neve J, Polla M, Quinn R): Use of cyclic anabaenopeptin-type peptides for the treatment of a condition wherein inhibition of carboxypeptidase U is beneficial, novel anabaenopeptin derivatives and intermediates thereof. WO-05039617 (2005).
    • ASTRAZENECA AB (Björquist P, Buchanan M, Campitelli M, Carroll A, Hyde E, Neve J, Polla M, Quinn R): Use of cyclic anabaenopeptin-type peptides for the treatment of a condition wherein inhibition of carboxypeptidase U is beneficial, novel anabaenopeptin derivatives and intermediates thereof. WO-05039617 (2005).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.