Flow cytometric measurement of kinetic and equilibrium binding parameters of arginine-glycine-aspartic acid ligands in binding to glycoprotein IIb/IIIa on platelets

Cytometry

Volumn 28, Issue 1, 1997, Pages 58-65

  Bednar, Bohumil ^a   Cunningham, Michael E ^a   McQueney, Patricia A ^a   Egbertson, Melissa S ^a   Askew, Benny C ^a   Bednar, Rodney A ^a   Hartman, George D ^a   Gould, Robert J ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Fibrinogen; Flow cytometry methods; Fluorescent RGD peptidomimetics; Glycoprotein IIb IIIa; Ligand binding; Receptor antagonists

Indexed keywords

FIBRINOGEN RECEPTOR; FIBRINOGEN RECEPTOR ANTAGONIST; L 762745; L 769434; N [(4 METHYLPHENYL)SULFONYL] 3 [[[5,6,7,8 TETRAHYDRO 4 OXO 5 [2 (4 PIPERIDINYL)ETHYL] 4H PYRAZOLO[1,5 A][1,4]DIAZEPIN 2 YL]CARBONYL]AMINO]ALANINE; PEPTIDOMIMETIC AGENT; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; FLOW CYTOMETRY; FLUORESCENCE; HUMAN; HUMAN CELL; KINETICS; LIGAND BINDING; NORMAL HUMAN; PREVENTION; PRIORITY JOURNAL; THROMBOCYTE AGGREGATION;

BINDING, COMPETITIVE; FLOW CYTOMETRY; FLUORESCENT DYES; HUMANS; KINETICS; LIGANDS; OLIGOPEPTIDES; PLATELET AGGREGATION INHIBITORS; PLATELET GLYCOPROTEIN GPIIB-IIIA COMPLEX; PROTEIN BINDING; RECEPTORS, IMMUNOLOGIC;

EID: 0030917144     PISSN: 01964763     EISSN: None     Source Type: Journal    
DOI: 10.1002/(SICI)1097-0320(19970501)28:1<58::AID-CYTO7>3.0.CO;2-D     Document Type: Article

References (24)

1. Bennett JS, Shatil SJ, Power JW, Gartner TK: Interaction of fibrinogen with its platelet receptor: Differential effects of α and γ chain fibrinogen peptides on the glycoprotein IIb/IIIa complex. J Biol Chem 263:9480-953, 1988.
2. 3, the fibrinogen receptor. Proc Soc Exp Biol Med 208:346-360, 1995.
3. Cook NS, Kottirsch G, Zerwes H-G: Platelet glycoprotein IIb/IIIa antagonists. Drugs Future 19:135-159, 1994.
4. Egbertson MS, Chang CT-C, Duggan ME, Gould RJ, Halczenko W, Hartman GD, Laswell WL, Lynch JJ, Lynch RJ, Manno PM, Naylor AM, Prgh JD, Ramjit DR, Sitko GR, Smith RS, Turchi LM, Zang G: Nonpeptide fibrinogen receptor antagonists. 2. Optimization of tyrosine template as a mimic for Arg-Gly-Asp. J Med Chem 37:2137-2551, 1994.
5. Egbertson MS, Bednar B, Bednar RA, Hartman GD, Gould RJ, Lynch RJ, Vassallo LM, Young SD: Nonpeptide glycoprotein IIb/IIIa inhibitors. 9. Centrally constrained alpha-sulfonamides are useful tools for exploring platelet receptor function. Bioorg Med Chem Lett 6:1415-1420, 1996.
6. Farell DH, Thiagarajan P, Chung DW, Davie EW: Role of fibrinogen α and γ chain sites in platelet aggregation. Proc Natl Acad Sci USA 89:729-732, 1992.
7. Fay SP, Posner RG, Swann WN, Sklar LA: Real-time analysis of the assembly of ligand, receptor, and G protein by quantitative fluorescence flow cytometry. Biochemistry 30:5066-5075, 1991.
8. Frelinger AL, Lam SC-T, Plow EF, Smith MA, Loftus JC, Ginsberg MH: Occupancy of adhesive protein receptor modulates expression of an antigenic site involved in cell adhesion. J Biol Chem 263:12397-12402, 1988.
9. Gan Z-R, Gould RJ, Jacobs JW, Friedman PA, Polokoff MA: Echistatin. A potent platelet aggregation inhibitor from the venom of the viper, Echis carinatus. J Biol Chem 263:19827-19832, 1988.
10. Gould RJ, Pollokoff MA, Friedman PA, Huang T-F, Holt JC, Cook JJ, Niewiarowski S: Disintegrins: A family of integrin inhibitory proteins from viper venoms. Proc Soc Exp Biol Med 195:168-171, 1990.
11. Heilmann E, Hyne LA, Burstein SA, George JN, Dale GL: Fluorescein derivatization of fibrinogen for flow cytometric analysis of fibrinogen binding to platelets. Cytometry 17:287-293, 1994.
12. Huber W, Schlatter D, Barner R, Hubscher J, Kouns WC, Steiner B: Determination of kinetic constants for interaction between the platelet glycoprotein IIb-IIIa and fibrinogen by means of surface plasmon resonance. Eur J Biochem 227:647-656, 1995.
13. Hulme EC, Birdsall NJ: Strategy and tactics in receptor-binding studies. In: Receptor-Ligand Interactions, Hulme EC (ed). Oxford University Press, Oxford, 1992, pp 66-177.
14. Kerker M, VanDilla MA, Brunsting A, Kratohvil JP, Hsu P, Wang DS, Gray JW, Langlois RC: Is the central dogma of flow cytometry true: The fluorescence intensity is proportional to cellular dye content? Cytometry 3:71-78, 1982.
15. Kieffer N, Phillips DR: Platelet membrane glycoproteins: Functions in cellular interactions. Annu Rev Cell Biol 6:329-357, 1990.
16. Kouns WC, Kircghofer D, Harvary P, Edunhofer A, Weller T, Pfenninger G, Baumgartner HR, Jennings LK, Steiner B: Reversible conformational changes induced in glycoprotein IIb-IIIa by potent and selective peptidomimetic inhibitors. Blood 80:2539-2547, 1992.
17. Lefkovits I, Plow EF, Topol EJ: Platelet glycoprotein IIb/IIIa receptor in cardiovascular medicine. N Eng J Med 332:1553-1559, 1993.
18. Liu C-Z, Wang Y-W, Shen M-C, Huang T-F: Analysis of human platelet glycoprotein IIb-IIIa by fluorescein isothiocyanate-conjugate disintegrins with flow cytometry. Thromb Haemostasis 72:919-925, 1994.
19. Muller B, Zerwes H-G, Tangemann K, Peter J, Engel J: Two step binding mechanism of fibrinogen to αIIbβ3 integrin reconstituted into planar lipid bilayers. J Biol Chem 268:6800-6808, 1993.
20. Phillips DR, Charo IF, Parise LV, Fitzgerald LA: The platelet membrane glycoprotein IIB-IIIa Complex. Blood 71:831-843, 1988.
21. Prueksaritanont T, Gorham LM, Naue JA, Hamill TG, Askew BC, Vyas KP: Disposition of L-738,167, a potent and long acting fibrinogen receptor antagonist, in dogs: Dose-dependent pharmacokinetics. Drug Metab Dispos 25:, 1997 (in press).
22. Tsao PW, Bozarth JM, Jackson SA, Forsythe MS, Flint SK, Mousa SA: Platelet GPIIb/IIIa receptor occupancy studies using a novel fluoresceinated cyclic ARG-GLY-ASP peptide. Thromb Res 77:543-556, 1995.
23. Weiland GA, Molinoff PB: Quantitative analysis of drug-receptor interactions: I. Determination of kinetic and equilibrium properties. Life Sci 29:313-330, 1981.
24. Weiss FJ, Bray PF, Tayback M, Schulman SP, Kickler TS, Becker LC, Weiss JL, Gerstenblith G, Goldschmidt-Clermont P: A polymorphism of platelet glycoprotein receptor as an inherited risk factor for coronary thrombosis. N Engl J Med 334:1090-1094, 1996.