The integrin αIIβ3 (GPIIb/IIIa): A target for novel anti-platelet drugs

Pharmacology Reviews and Communications

Volumn 8, Issue 4, 1996, Pages 257-265

  Feuerstein, Giora ^a   Ruffolo Jr , Robert R ^a   Samanen, James ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

Fibrinogen receptor; Glycoprotein IIb IIIa; Integrin; Myocardial infarction; Platelet; Stroke; Thrombosis

Indexed keywords

EID: 0344245199     PISSN: 10288945     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (34)

1. Steering Committee of the Physicians' Health Study Research Group (1989). Final Report on the Aspirin Component of the Ongoing Physicians' Health Study, New England Journal of Medicine, 321, 129-135.
2. ISIS-2 (Second International Study of Infarct Survival) Collaborative Group (1988). Randomized trial of intravenous streptokinase, oral aspirin, both, or neither among 17,187 cases of suspected acute myocardial infarctions: ISIA-2, Lancet, 2, 349-360.
3. UK-TIA Study Group, (1988). United Kingdom transient ischaemic attack (UK-TIA) aspirin trial: interim results, British Medical Journal, 296, 316-320.
4. The EPIC Investigators, (1994). Use of a Monoclonal Antibody Directed Against the Platelet Glycoprotein IIb/IIIa Receptor in High-Risk Coronary Angioplasty, The New England Journal of Medicine, 330, 956-961.
5. Bennett, J. S. and Vilaire, G. (1979). Exposure of Platelet Fibrinogen Receptors by ADP and Epinephrine, Journal Clinical Investigators, 64, 1393.
6. Margtierie, G. A., Plow, E. F. and Edgington, T. S. (1979). Human Platelets Possess an Inducible and Saturable Receptor Specific for Fibrinogen, Journal of Biological Chemistry, 254, 5357-5363.
7. Hawiger, J., Parkinson, S. and Timmons, S. (1980). Prostacyclin inhibits mobilisation of fibrinogen-binding sites on human ADP- and thrombin-treated platelets, Nature, 283, 195.
8. Shatfil, S. J., Hoxie, J. A., Cunningham, M. and Brass, L. F. (1985). Changes in the Platelet Membrand Glycoprotein IIb/IIIa Complex during Platelet Activation, The Journal of Biological Chemistry, 260, 11107-11114.
9. Coller, B. S. (1985). A New Murine Monoclonal Antibody Reports an Activation-dependent Change in the Conformation and/or Microenvironment of the Platelet Glycoprotein IIb/IIIa Complex, The American Society for Clinical Investigation, Inc, 76, 101-108.
10. Parise, L. V., Heigerson, S. L., Steiner, B., Nanniai, L. and Phillips, D. R. (1987). Synthetic Peptides Derived from Fibrinogen and Fibronectin Change the Conformation of Purified Platelet Glycoprotein IIb/IIIa, The Journal of Biological Chemistry, 262, 12597-12602.
11. Feuerstein, G. and Ruffolo, R. R. (1994). Ticlopidine: a novel antiplatelet drug for prevention of thrombobc disorders, Expert Opinion lnvestigational Drugs, 3, 1163-1169.
12. Cheresh, D. A., Berliner, S. A., Vicente, V. and Ruggeri, Z. M. (1989). Recognition of Distinct Adhesive Sites on Fibrinogen by Related Integrins on Platelets and Endothelial Cells, Cell, 58, 945-953.
13. Farrell, D. H., Thiagarajan, P., Chung, D. W. and Davie, E. W. (1992). Role of fibrinogen α and γ chain sites in platelet aggregation, Procedures National Academy of Sciences, USA, 89, 10729-10732.
14. Gould, R. J., Polokoff, M. A., Friedman, P. A., Huang, T-E., Holt, J. C., Cook, J. J. and Niewiarowski, S. (1990). Disintegrins: A Family of Integrin Inhibitory Proteins from Viper Venoms (43129 B), Procedings of the Society for Experimental Biology and Medicine, 195, 168-171.
15. Huang, T.-F., Holt, J. C., Lukasiewicz, H. and Niewiarowski, S. (1987). Trigramin A Low Molecular Weight Peptide Inhibiting Fibrinogen Interaction With Platelet Receptors Expressed on Glycoprotein IIb/IIIa Complex, Journal of Biological Chemistry, 262, 16157-16163.
16. Dennis, M. S., Carter, P. and Lazams, R. A. (1993). Binding Interactions of Kistrin With Platelet Glycoprotein lib-IHa: Analysis by Site-Directed Mutagenesis, Proteins: Structure, Function, and Genetics, 15, 312-321.
17. Beacham, D. A., Wise, R. J., Turci, S. M. and Handin, R. I. (1992). Selective Inactivation of the Arg-Gly-Asp-Ser (RGDS) Binding Site in von Willebrand Factor by Site-directed Mutagenesis, Journal of Biological Chemistry, 267, 3409.
18. Yarnada, T., Matsushima, M., Inaka, K., Ohkubo, T., Uyeda, A., Maeda, T., Titani, K, Sekiguchi, K. and Kikuchi, M., (1993). Structural and Functional Analyses of the Arg-Gly-Asp Sequence Introduced into Human Lysozyme. The Journal of Biological Chemistry, 268, 10588.
19. Lee, G., Chan, W., Hurle, M. R., Desjarlais, R., Watson, F., Sathe, G. M., Wetzel, R. (1993). Strong inhibition of fibrinogen binding to platelet receptor allbb3 by RGD sequences installed into a presentation scaffold, Protein Engineering, 6, 745.
20. Timmons, S., Bednatek, M. A., Klmzewiak, M. and Hawiger, J. (1989). Antiplatelet "Hybrid" Peptides Analogous to Receptor Recognition Domains on γ and α. Chains of Human Fibrinogen, Biochemistry, 28, 2919.
21. Kloczewiak, M., Timmons, S., Bednarek, M. A., Sakon, M. and Hawiger, J. (1989). Platelet Receptor Recognition Domain on the γ Chain of Human Fibrinogen and Its Synthetic Peptide Analogues, Biochemistry, 28, 2915-2919.
22. Hawiger, J., Kloczewiak, M., Bednarek, M. A. and Timmons, S. (1989). Platelet Receptor Recognition Domains on the α Chain of Human Fibrinogen: Structure-Function Analysis, Biochemistry, 28, 2909-2914.
23. Coller, B. S., Folts, J. D., Smith, S. R., Scudder, I. F. and Jordan, R. (1989). Abolition of In Vivo Platelet Thrombus Formation in Primates With Monoclonal Antibodies to the Platelet GpIIb/IIIa Receptor, Circulation, 80, 1766.
24. Coller, B. S., Folts, J. D., Scudder, L E. and Smith, S. R. (1986). Antithrombolic Effect of a Monoclonal Antibody to the Platelet Glycoprotein IIb/IIIa Receptor in an Experimental Animal Model, Blood, 68, 783.
25. Hanson, S. R., Pareti, F. I., Ruggeri, Z. M., Marzec, U. M., Kunicki, T. J., Montgomery, R. R., Zimmerman, T. S. and Harker, L. A. (1998). Effects of Monoclonal Antibodies against the Platelet Glycoprotein IIb/IIIa Complex on Thrombosis and Hemostasis in the Baboon, Journal of Clinical Investigators, 81, 149.
26. Hartman, G. D., Egbertson, M. S., Hakzenko, W., Laswell, W. L., Duggan, M. E., Smith, R. L., Naylor, A. M., Manno, P. D., Lynch, R. J., Zhang, G. X., Chang, C. T. C. and Gould, R. J. (1992). Non-Pepride Fibrinogen Receptor Antagonists. 1. Discovery and Design of Exosite Inhibitors, Journal of Medicinal Chemistry, 35, 4640.
27. Ku, T. W., Ali, F. E., Barton, L. S., Bean, I. W., Bondinell, W. E., Burgess, J. L., Callahan, J. F., Calvo, R. R., Chen, L. C., Eggleston, D. S., Gleason, J. C., Hoffman, W. F., Hwang, S. M., Jakas, D. R., Karash, C. B., Keenan, R. M., Kopple, K. D., Miller, W. H., Newlander, K. A., Nichols, A., Parker, M. F., Peishoff, C. E., Samanen, J. M., Uzinskas, I. and Venslavsky, J. W. (1993). Direct Design of a Potent Non-Pepride Fibrinogen Receptor Antagonist Based on the Structure and Conformation of a Highly Constrained Cyclic RGD Peptide, Journal of American Chemical Society, 115, 8861-8862.
28. Ku, T. W., Ali, F. E., Barton, L. S., Bean, J. W., Bondinell, W. E., Burgess, J. L., Callahan, J. F., Calvo, R. R., Chen, L., Eggleslon, D S., Gleason, J. G., Hoffman, W. F., Hwang, S., Jakas, D. R., Karash, C. B., Keenan, R. M., Kopple, K. D., Miller, W. M., Newlander, K. A., Nichols, A., Parker, M. F., Peishoff, C. E., Samanen, J. M., Uzinskas, I. and Venslavsky, J. W. (1993). Direct Design of a Potent Non-Peptide Fibrinogen Receptor Antagonist Based on the Structure and Conformation of a Highly Contrained Cyclic RGD Peptide, J. Amer. Chem. Soc., 115, 8861-8862.
29. Frishman, W. H., Burns, B., Atac, B., Alturk, N., Altajar, B. and Lerrick, K (1995). Novel Antiplatelet Therapies for Treatment of Patients with Ischemic Heart Disease: Inhibitors of the Platelet Glycoprotein IIb/IIIaIntegrin Receptor, Am. Heart J., 130, 877-892.
30. Mousa, S. A., Bozarth, J. M., Forsythe, M. S., Jackson, S. M, Leamy, A., Diemer, M M., Kapit, R. P., Knabb, R. M., Mayo, M. C., Pierce, S. K., DeGrado, W. F., Thoolen, M. J. and Reilly, T. M. (1994). Antiplatelet and Antithrombotic Efficacy of DMP728, a Novel Platelet GPIIb/IIIa Receptor Antagonist, Circulation, 89, 3.
31. Yasuda, T., Gold, H. K, Kohmura, C., Guerrero, L., Yaoita, H., Fallon, J. T., Bunting, S. and Collen, D. (1993). Intravenous and Endobronchial Administration of G4120, a Cyclic Arg-Gly-Asp-Containing Platelet GpIIb/IIIa Receptor-Blocking Pentapeptide, Enhances and Sustains Coronary Arterial Thrombolysis With rt-PA in a Canine Preparation, Arteriosclerosis and Thrombosis, 13, 738-747.
32. Roux, S. P., Tschopp, T. B., Kuhn, H., Steiner, B. and Hadvary, P. (1993). Effects of Heparin, Aspirin and a Synthetic Platelet Glycoprotein IIb-IIIa Receptor Antagonist (Ro 43-5054) on Coronary Artery Reperfusion and Reocclusion after Thrombolysis with Tissue-Type Plasminogen Activator in the Dog, The Journal of Pharmacology and Experimental Therapeutics, 264, 501-508.
33. Ferguson, J. J. (1996). EPILOG and CAPTURE Trials Halted Because of Positive Interim Results, Circulation, 93, 637.
34. Lefkovits, M. B., Plow, E. F., Topol, E. J. (1995). Platelet Glycoprotein IIb/IIIa Receptors in Cardiovascular Medicine, The New England Journal of Medicine, 332, 1553-1559.