653
Views
2
CrossRef citations to date
0
Altmetric
CURRENT CLINICAL PRACTICE: HEMOSTASIS

Protein anticoagulants targeting factor VIIa–tissue factor complex: a comprehensive review

, &

References

  • Davie EW, Fujikawa K, Kisiel W. The coagulation cascade: initiation, maintenance, and regulation. Biochemistry. 1991;30(43):10363–70.
  • Edgington TS, Dickinson CD, Ruf W. The structural basis of function of the TF. VIIa complex in the cellular initiation of coagulation. Thromb Haemost. 1997;78(1):401–5.
  • Al-Amoudi SM. Anticoagulant induced leukoagglutination. Saudi Med J. 2008;29(8):1192–3.
  • Felmeden DC, Spencer CG, Chung NA, Belgore FM, Blann AD, Beevers DG, et al. Relation of thrombogenesis in systemic hypertension to angiogenesis and endothelial damage/dysfunction (a substudy of the Anglo-Scandinavian Cardiac Outcomes Trial [ASCOT]). Am J Cardiol. 2003;92(4):400–5.
  • Napoleone E, Di SA, Camera M, Tremoli E, Lorenzet R. Angiotensin-converting enzyme inhibitors downregulate tissue factor synthesis in monocytes. Circ Res. 2000;86(2):139–43.
  • Boeri D, Almus FE, Maiello M, Cagliero E, Rao LV, Lorenzi M. Modification of tissue-factor mRNA and protein response to thrombin and interleukin 1 by high glucose in cultured human endothelial cells. Diabetes. 1989;38(2):212–8.
  • Aljada A, Ghanim H, Mohanty P, Kapur N, Dandona P. Insulin inhibits the pro-inflammatory transcription factor early growth response gene-1 (Egr)-1 expression in mononuclear cells (MNC) and reduces plasma tissue factor (TF) and plasminogen activator inhibitor-1 (PAI-1) concentrations. J Clin Endocrinol Metab. 2002;87(3):1419–22.
  • Wada H, Kaneko T, Wakita Y, Minamikawa K, Nagaya S, Tamaki S, et al. Effect of lipoproteins on tissue factor activity and PAI-II antigen in human monocytes and macrophages. Int J Cardiol. 1994;47 (Suppl 1):S21–5.
  • Matetzky S, Tani S, Kangavari S, Dimayuga P, Yano J, Xu H, et al. Smoking increases tissue factor expression in atherosclerotic plaques: implications for plaque thrombogenicity. Circulation. 2000;102(6):602–4.
  • Hansson GK. Inflammation, atherosclerosis, and coronary artery disease. N Engl J Med. 2005;352(16):1685–95.
  • Annex BH, Denning SM, Channon KM, Sketch MH, Stack RS, Morrissey JH, et al. Differential expression of tissue factor protein in directional atherectomy specimens from patients with stable and unstable coronary syndromes. Circulation. 1995;91(3):619–22.
  • Wilcox JN, Smith KM, Schwartz SM, Gordon D. Localization of tissue factor in the normal vessel wall and in the atherosclerotic plaque. Proc Natl Acad Sci USA. 1989;86(8):2839–43.
  • Kaikita K, Ogawa H, Yasue H, Takeya M, Takahashi K, Saito T, et al. Tissue factor expression on macrophages in coronary plaques in patients with unstable angina. Arterioscler Thromb Vasc Biol. 1997;17(10):2232–7.
  • Erlich JH, Holdsworth SR, Tipping PG. Tissue factor initiates glomerular fibrin deposition and promotes major histocompatibility complex class II expression in crescentic glomerulonephritis. Am J Pathol. 1997;150(3):873–80.
  • Erlich JH, Boyle EM, Labriola J, Kovacich JC, Santucci RA, Fearns C, et al. Inhibition of the tissue factor-thrombin pathway limits infarct size after myocardial ischemia-reperfusion injury by reducing inflammation. Am J Pathol. 2000;157(6):1849–62.
  • Himber J, Wohlgensinger C, Roux S, Damico LA, Fallon JT, Kirchhofer D, et al. Inhibition of tissue factor limits the growth of venous thrombus in the rabbit. J Thromb Haemost. 2003;1(5):889–95.
  • Taylor FB, Chang A, Ruf W, Morrissey JH, Hinshaw L, Catlett R, et al. Lethal E. coli septic shock is prevented by blocking tissue factor with monoclonal antibody. Circ Shock. 1991;33(3):127–34.
  • Al-Nozha MM, Abdel-Gader AG, Arafah MR, Al-Maatouq MA, Al-Shahid MS, Al-Harthi SS, et al. Tissue factor pathway inhibitor, natural coagulation inhibitors and hemostatic activation markers in patients with acute coronary syndromes. Saudi Med J. 2005;26(6):937–42.
  • Lwaleed BA. Tissue factor: biological function and clinical significance. Saudi Med J. 2002;23(2):135–43.
  • Coughlin SR. Thrombin signalling and protease-activated receptors. Nature. 2000;407(6801):258–64.
  • Ndonwi M, Tuley EA, Broze GJ The Kunitz-3 domain of TFPI-alpha is required for protein S-dependent enhancement of factor Xa inhibition. Blood. 2010;116(8):1344–51.
  • Bajaj MS, Birktoft JJ, Steer SA, Bajaj SP. Structure and biology of tissue factor pathway inhibitor. Thromb Haemost. 2001;86(4):959–72.
  • Hamamoto T, Yamamoto M, Nordfang O, Petersen JG, Foster DC, Kisiel W. Inhibitory properties of full-length and truncated recombinant tissue factor pathway inhibitor (TFPI). Evidence that the third Kunitz-type domain of TFPI is not essential for the inhibition of factor VIIa-tissue factor complexes on cell surfaces. J Biol Chem. 1993;268(12):8704–10.
  • Burgering MJ, Orbons LP, van der Doelen A, Mulders J, Theunissen HJ, Grootenhuis PD, et al. The second Kunitz domain of human tissue factor pathway inhibitor: cloning, structure determination and interaction with factor Xa. J Mol Biol. 1997;269(3):395–407.
  • Mine S, Yamazaki T, Miyata T, Hara S, Kato H. Structural mechanism for heparin-binding of the third Kunitz domain of human tissue factor pathway inhibitor. Biochemistry. 2002;41(1):78–85.
  • Baugh RJ, Broze GJ, Krishnaswamy S. Regulation of extrinsic pathway factor Xa formation by tissue factor pathway inhibitor. J Biol Chem. 1998;273(8):4378–86.
  • Panteleev MA, Zarnitsina VI, Ataullakhanov FI. Tissue factor pathway inhibitor: a possible mechanism of action. Eur J Biochem. 2002;269(8):2016–31.
  • Petersen LC, Bjorn SE, Olsen OH, Nordfang O, Norris F, Norris K. Inhibitory properties of separate recombinant Kunitz-type-protease-inhibitor domains from tissue-factor-pathway inhibitor. Eur J Biochem. 1996;235(1–2):310–6.
  • Girard TJ, MacPhail LA, Likert KM, Novotny WF, Miletich JP, Broze GJ. Inhibition of factor VIIa-tissue factor coagulation activity by a hybrid protein. Science. 1990;248(4961):1421–4.
  • Abraham E, Reinhart K, Svoboda P, Seibert A, Olthoff D, Dal NA, et al. Assessment of the safety of recombinant tissue factor pathway inhibitor in patients with severe sepsis: a multicenter, randomized, placebo-controlled, single-blind, dose escalation study. Crit Care Med. 2001;29(11):2081–9.
  • Abraham E, Reinhart K, Opal S, Demeyer I, Doig C, Rodriguez AL, et al. Efficacy and safety of tifacogin (recombinant tissue factor pathway inhibitor) in severe sepsis: a randomized controlled trial. JAMA. 2003;290(2):238–47.
  • Petersen LC, Sprecher CA, Foster DC, Blumberg H, Hamamoto T, Kisiel W. Inhibitory properties of a novel human Kunitz-type protease inhibitor homologous to tissue factor pathway inhibitor. Biochemistry. 1996;35(1):266–72.
  • Holst J, Lindblad B, Bergqvist D, Nordfang O, Ostergaard PB, Petersen JG, et al. Antithrombotic effect of recombinant truncated tissue factor pathway inhibitor (TFPI1–161) in experimental venous thrombosis – a comparison with low molecular weight heparin. Thromb Haemost. 1994;71(2):214–9.
  • Cappello M, Vlasuk GP, Bergum PW, Huang S, Hotez PJ. Ancylostoma caninum anticoagulant peptide: a hookworm-derived inhibitor of human coagulation factor Xa. Proc Natl Acad Sci USA. 1995;92(13):6152–6.
  • Duggan BM, Dyson HJ, Wright PE. Inherent flexibility in a potent inhibitor of blood coagulation, recombinant nematode anticoagulant protein c2. Eur J Biochem. 1999;265(2):539–48.
  • Lee AY, Vlasuk GP. Recombinant nematode anticoagulant protein c2 and other inhibitors targeting blood coagulation factor VIIa/tissue factor. J Intern Med. 2003;254(4):313–21.
  • Lee A, Agnelli G, Buller H, Ginsberg J, Heit J, Rote W, et al. Dose-response study of recombinant factor VIIa/tissue factor inhibitor recombinant nematode anticoagulant protein c2 in prevention of postoperative venous thromboembolism in patients undergoing total knee replacement. Circulation. 2001;104(1):74–8.
  • Giugliano RP, Wiviott SD, Stone PH, Simon DI, Schweiger MJ, Bouchard A, et al. Recombinant nematode anticoagulant protein c2 in patients with non-ST-segment elevation acute coronary syndrome: the ANTHEM-TIMI-32 trial. J Am Coll Cardiol. 2007;49(25):2398–407.
  • Monteiro RQ, Rezaie AR, Ribeiro JM, Francischetti IM. Ixolaris: a factor Xa heparin-binding exosite inhibitor. Biochem J. 2005;387(Pt 3):871–7.
  • Carneiro-Lobo TC, Konig S, Machado DE, Nasciutti LE, Forni MF, Francischetti IM, et al. Ixolaris, a tissue factor inhibitor, blocks primary tumor growth and angiogenesis in a glioblastoma model. J Thromb Haemost. 2009;7(11):1855–64.
  • Bode W, Huber R. Natural protein proteinase inhibitors and their interaction with proteinases. Eur J Biochem. 1992;204(2):433–51.
  • Dennis MS, Lazarus RA. Kunitz domain inhibitors of tissue factor-factor VIIa. I. Potent inhibitors selected from libraries by phage display. J Biol Chem. 1994;269(35):22129–36.
  • Lee GF, Lazarus RA, Kelley RF. Potent bifunctional anticoagulants: Kunitz domain-tissue factor fusion proteins. Biochemistry. 1997;36(19):5607–11.
  • Stassen JM, Lambeir AM, Matthyssens G, Ripka WC, Nystrom A, Sixma JJ, et al. Characterisation of a novel series of aprotinin-derived anticoagulants. I. In vitro and pharmacological properties. Thromb Haemost. 1995;74(2):646–54.
  • Zhang E, St CR, Tulinsky A. Structure of extracellular tissue factor complexed with factor VIIa inhibited with a BPTI mutant. J Mol Biol. 1999;285(5):2089–104.
  • Stassen JM, Lambeir AM, Vreys I, Deckmyn H, Matthyssens G, Nystrom A, et al. Characterisation of a novel series of aprotinin-derived anticoagulants. II. Comparative antithrombotic effects on primary thrombus formation in vivo. Thromb Haemost. 1995;74(2):655–9.
  • Taylor FB Role of tissue factor and factor VIIa in the coagulant and inflammatory response to LD100 Escherichia coli in the baboon. Haemostasis. 1996;26 (Suppl 1):83–91.
  • Nemerson Y, Gentry R. An ordered addition, essential activation model of the tissue factor pathway of coagulation: evidence for a conformational cage. Biochemistry. 1986;25(14):4020–33.
  • Sorensen BB, Persson E, Freskgard PO, Kjalke M, Ezban M, Williams T, et al. Incorporation of an active site inhibitor in factor VIIa alters the affinity for tissue factor. J Biol Chem. 1997;272(18):11863–8.
  • Jang Y, Guzman LA, Lincoff AM, Gottsauner-Wolf M, Forudi F, Hart CE, et al. Influence of blockade at specific levels of the coagulation cascade on restenosis in a rabbit atherosclerotic femoral artery injury model. Circulation. 1995;92(10):3041–50.
  • Roy S, Hass PE, Bourell JH, Henzel WJ, Vehar GA. Lysine residues 165 and 166 are essential for the cofactor function of tissue factor. J Biol Chem. 1991;266(32):22063–6.
  • Ruf W, Miles DJ, Rehemtulla A, Edgington TS. Cofactor residues lysine 165 and 166 are critical for protein substrate recognition by the tissue factor-factor VIIa protease complex. J Biol Chem. 1992;267(9):6375–81.
  • Dickinson CD, Shobe J, Ruf W. Influence of cofactor binding and active site occupancy on the conformation of the macromolecular substrate exosite of factor VIIa. J Mol Biol. 1998;277(4):959–71.
  • Biemond BJ, Levi M, ten CH, Soule HR, Morris LD, Foster DL, et al. Complete inhibition of endotoxin-induced coagulation activation in chimpanzees with a monoclonal Fab fragment against factor VII/VIIa. Thromb Haemost. 1995;73(2):223–30.
  • Pawashe AB, Golino P, Ambrosio G, Migliaccio F, Ragni M, Pascucci I, et al. A monoclonal antibody against rabbit tissue factor inhibits thrombus formation in stenotic injured rabbit carotid arteries. Circ Res. 1994;74(1):56–63.
  • Golino P, Ragni M, Cirillo P, Avvedimento VE, Feliciello A, Esposito N, et al. Effects of tissue factor induced by oxygen free radicals on coronary flow during reperfusion. Nat Med. 1996;2(1):35–40.
  • Huang M, Syed R, Stura EA, Stone MJ, Stefanko RS, Ruf W, et al. The mechanism of an inhibitory antibody on TF-initiated blood coagulation revealed by the crystal structures of human tissue factor, Fab 5G9 and TF.G9 complex. J Mol Biol. 1998;275(5):873–94.
  • Ragni M, Cirillo P, Pascucci I, Scognamiglio A, D'Andrea D, Eramo N, et al. Monoclonal antibody against tissue factor shortens tissue plasminogen activator lysis time and prevents reocclusion in a rabbit model of carotid artery thrombosis. Circulation. 1996;93(10):1913–8.
  • Badimon JJ, Lettino M, Toschi V, Fuster V, Berrozpe M, Chesebro JH, et al. Local inhibition of tissue factor reduces the thrombogenicity of disrupted human atherosclerotic plaques: effects of tissue factor pathway inhibitor on plaque thrombogenicity under flow conditions. Circulation. 1999;99(14):1780–7.
  • Morrow DA, Murphy SA, McCabe CH, Mackman N, Wong HC, Antman EM. Potent inhibition of thrombin with a monoclonal antibody against tissue factor (Sunol-cH36): results of the PROXIMATE-TIMI 27 trial. Eur Heart J. 2005;26(7):682–8.
  • Cavusoglu E, Chen I, Rappaport J, Marmur JD. Inhibition of tissue factor gene induction and activity using a hairpin ribozyme. Circulation. 2002;105(19):2282–7.
  • Stephens AC, Rivers RP. Suppression of human monocyte tissue factor synthesis by antisense oligodeoxynucleotide. Thromb Res. 1997;85(5):387–98.
  • Dennis MS, Eigenbrot C, Skelton NJ, Ultsch MH, Santell L, Dwyer MA, et al. Peptide exosite inhibitors of factor VIIa as anticoagulants. Nature. 2000;404(6777):465–70.
  • Roberge M, Santell L, Dennis MS, Eigenbrot C, Dwyer MA, Lazarus RA. A novel exosite on coagulation factor VIIa and its molecular interactions with a new class of peptide inhibitors. Biochemistry. 2001;40(32):9522–31.
  • Eigenbrot C, Kirchhofer D, Dennis MS, Santell L, Lazarus RA, Stamos J, et al. The factor VII zymogen structure reveals reregistration of beta strands during activation. Structure. 2001;9(7):627–36.
  • Orning L, Fischer PM, Hu CK, Agner E, Engebretsen M, Husbyn M, et al. A cyclic pentapeptide derived from the second EGF-like domain of Factor VII is an inhibitor of tissue factor dependent coagulation and thrombus formation. Thromb Haemost. 2002;87(1):13–21.
  • Banerjee Y, Mizuguchi J, Iwanaga S, Kini RM. Hemextin AB complex, a unique anticoagulant protein complex from Hemachatus haemachatus (African Ringhals cobra) venom that inhibits clot initiation and factor VIIa activity. J Biol Chem. 2005;280(52):42601–11.
  • Banerjee Y, Mizuguchi J, Iwanaga S, Kini RM. Hemextin AB complex – a snake venom anticoagulant protein complex that inhibits factor VIIa activity. Pathophysiol Haemost Thromb. 2005;34(4–5):184–7.
  • Banerjee Y, Lakshminarayanan R, Vivekanandan S, Anand GS, Valiyaveettil S, Kini RM. Biophysical characterization of anticoagulant hemextin AB complex from the venom of snake Hemachatus haemachatus. Biophys J. 2007;93(11):3963–76.
  • Miller DG, Adam MA, Miller AD. Gene transfer by retrovirus vectors occurs only in cells that are actively replicating at the time of infection. Mol Cell Biol. 1990;10(8):4239–42.
  • Cone RD, Mulligan RC. High-efficiency gene transfer into mammalian cells: generation of helper-free recombinant retrovirus with broad mammalian host range. Proc Natl Acad Sci USA. 1984;81(20):6349–53.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.