Binding of a thrombin receptor tethered ligand analogue to human platelet thrombin receptor

Molecular Pharmacology

Volumn 51, Issue 2, 1997, Pages 350-356

  Ahn, Ho Sam ^a   Foster, Carolyn ^a   Boykow, George ^a   Arik, Leyla ^a   Smith Torhan, April ^a   Hesk, David ^a   Chatterjee, Meeta ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANGIOTENSIN; BRADYKININ; GUANINE NUCLEOTIDE BINDING PROTEIN; GUANOSINE TRIPHOSPHATE DERIVATIVE; GUANYLYLIMIDODIPHOSPHATE; NEUROKININ A; RADIOLIGAND; SUBSTANCE P; THROMBIN RECEPTOR; THROMBIN RECEPTOR ACTIVATING PEPTIDE; VASOACTIVE INTESTINAL POLYPEPTIDE;

ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; DISSOCIATION CONSTANT; DRUG BINDING SITE; DRUG POTENCY; DRUG RECEPTOR BINDING; HUMAN; HUMAN CELL; LIGAND BINDING; PRIORITY JOURNAL; THROMBOCYTE AGGREGATION; THROMBOCYTE MEMBRANE;

EID: 0031017203     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.51.2.350     Document Type: Article

References (39)

1. Vu, T. K. H., D. T. Hung, V. I. Wheaton, and S. R. Coughlin. Molecular cloning of a functional thrombin receptor reveals a novel proteolytic mechanism of receptor activation. Cell 64:1057-1068 (1991).
2. 2+ mobilization. FEBS Lett. 288:123-128 (1991).
3. Coughlin, S. R., T. K. H. Vu, D. T. Hung, and V. I. Wheaton. Characterization of a functional thrombin receptor. Issues and opportunities. J. Clin. Invest. 89:351-355 (1992).
4. Scarborough, R. M., M. A. Naughton, W. Teng, D. T. Hung, J. Rose, T. K. H. Vu, V. I. Wheaton, C. W. Turck, and S. R. Coughlin. Tethered ligand agonist peptides. Structural requirements for thrombin receptor activation reveal mechanism of proteolytic unmasking of agonist function. J. Biol. Chem. 267:13146-13149 (1992).
5. Vassallo, R. R., Jr., T. Kieber-Emmons, K. Cichowski, and L. F. Brass. Structure-function relationships in the activation of platelet thrombin receptors by receptor-derived peptides. J. Biol. Chem. 267:6081-6085 (1992).
6. Yang, S. G., A. Laniyonu, M. Saifeddine, G. J. Moore, and M. D. Hollenberg. Actions of thrombin and thrombin receptor peptide analogues in gastric and aortic smooth muscle. Development of bioassays for structure-activity studies. Life Sci. 51:1325-1332 (1992).
7. Antonaccio, M. J., D. Normandin, R. Serafino, and S. Moreland. Effects of thrombin and thrombin receptor-activating peptides on rat aortic vascular smooth muscle. J. Pharmacol. Exp. Ther. 266:125-132 (1993).
8. Albrightson, C. R., B. Zabko-Potapovich, G. Dytko, W. M. Bryan, K. Hoyle, M. L. Moore, and J. M. Stadel. Analogues of the thrombin receptor tethered-ligand enhance mesangial cell proliferation. Cell. Signal. 6:743-750 (1994).
9. Dennington, P. M., and M. C. Berndt. The thrombin receptor. Clin. Exp. Pharmacol. Physiol. 21:349-358 (1994).
10. Grand, R. J. A., A. S. Turnell, and P. W. Grabham. Cellular consequences of thrombin-receptor activation. Biochem. J. 313:353-368 (1996).
11. Huang, R.-S., A. Sorisky, W. R., Church, E. R. Simons, and S. Rittenhouse. "Thrombin" receptor-directed ligand accounts for activation by thrombin of platelet phospholipase C and accumulation of 3-phosphorylated phosphoinositides. J. Biol. Chem. 266:18435-18438 (1991).
12. Brass, L. F., J. A. Hoxie, T. Kieber-Emmons, D. R. Manning, M. Poncz, and M. Woolkalis. Agonist receptors and G proteins as mediators of platelet activation, in Mechanisms of Platelet Activation and Control (K. S. Authi, S. P. Watson and V. V. Kakkar, eds.). Academic Press, New York 17-36 (1993).
13. + exchange by a thrombin receptor antagonist. Biochem. Pharmacol. 49:519-528 (1995).
14. Pumiglia, K. M., and M. B. Feinstein. Thrombin and thrombin receptor agonist peptide induce tyrosine phosphorylation and tyrosine kinases in the platelet cytoskeleton. Biochem. J. 294:253-260 (1993).
15. Nelken, N. A., S. J. Soifer, J. O'Keefe, T. K. H. Vu, I. F. Charo, and S. R. Coughlin. Thrombin receptor expression in normal and atherosclerotic human arteries. J. Clin. Invest. 90:1614-1621 (1992).
16. Wilcox, J. N., J. Rodriguez, R. Subramanian, J. Ollerenshaw, C. Zhong, D. J. Hayzer, C. Horaist, S. R. Hanson, A. Lumsden, T. A. Salam, A. B. Kelly, L. A. Harker, and M. Runge. Characterization of thrombin receptor expression during vascular lesion formation. Circ. Res. 75:1029-1038 (1994).
17. Harker, L. A., S. R. Hanson, and M. Runge. Thrombin hypothesis of thrombus generation and vascular lesion formation. Am. J. Cardiol. 75: 12B-17B (1995).
18. 2+ mobilization. FEBS Lett. 288:123-128 (1991).
19. Seiler, S. M., M. Peluso, J. G. Tuttle, K. Pryor, C. Klimas, G. R. Matsueda, and M. S. Bernatowicz. Thrombin receptor activation by thrombin and receptor-derived peptides in platelet and CHRF-288 cell membranes: receptor-stimulated GTPase and evaluation of agonists and partial agonists Mol. Pharmacol. 49:190-197 (1996).
20. Cook, J. J., G. R. Sitko, B. Bednar, C. Condra, M. J. Mellott, D. -M. Feng, R. F. Nutt, J. A. Shafer, R. J. Gould, and T. M. Connolly. An antibody against the exosite of the cloned thrombin receptor inhibits experimental arterial thrombosis in the African green monkey. Circ. Res 91:2961-2971 (1995).
21. Feng, D.-M., D. F. Veber, T. M. Connolly, and R. F. Nutt. Novel thrombin receptor analogs with potent agonist effects, in Peptides: Chemistry, Structure and Biology, Proceedings of the Thirteenth American Peptide Symposium (R. S. Hodges and J. A. Smith, eds.). ESCOM, Leiden, The Netherlands, 387-389 (1994).
22. Feng, D.-M., D. F. Veber, T. M. Connolly, C. Condra, C., M.-J. Tang, and R. F. Nutt. Development of a potent thrombin receptor ligand. J. Med. Chem. 38:4125-4130 (1995).
23. Natarajan, S., D. Riexinger, M. Peluso, and S. M. Seiler. 'Tethered ligand' derived pentapeptide agonists of thrombin receptor: a study of side chain requirements for human platelet activation and GTPase stimulation. Int. J. Pept. Protein Res. 45:145-151 (1995).
24. Lowry, O. H., N. J. Rosebrough, A. L. Farr, and R. J. Randall. Protein measurement with the Folin phenol reagent. J. Biol. Chem. 193:265-275 (1951).
25. Bednar, B., C. Condra, R. J. Gould, and T. M. Connolly. Platelet aggregation monitored in a 96 well microplate reader is useful for evaluation of platelet agonists and antagonists. Thromb. Res. 77:453-463 (1995).
26. Nystedt, S., K. Emilsson, C. Wahlestedt, and J. Sundelin. Molecular cloning of a potential proteinase activated receptor. Proc. Natl. Acad. Sci. USA 91:9208-9212 (1994).
27. Chao, B. H., S. Kalkunte, J. M. Maraganore, and J. R. Stone. Essential groups in synthetic agonist peptides for activation of the platelet thrombin receptor. Biochemistry 31:6175-6178 (1992).
28. Sabo, T., D. Gurwitz, L. Motola, P. Brodt, R. Barak, and E. Elhanaty. Biochem. Biophys. Res. Commun. 188:604-610 (1992).
29. Hui, K. W., J. A. Jakubowski, V. L. Wyssm, and E. L. Angleton. Minimal sequence requirement of thrombin receptor agonist peptide. Biochem. Biophys. Res. Commun. 184:790-796 (1992).
30. Coughlin, S. R., and R. M. Scarborough. Recombinant thrombin receptor agonist and antagonist peptides, and (monoclonal) antibodies. World Patient 9214750A1 (PCT/US92/01312) (1992).
31. Esmon, C. T. Cell mediated events that control blood coagulation and vascular injury. Annu. Rev. Cell Biol. 9:1-26 (1993).
32. Cunningham, D. D., and D. H. Farrell. Thrombin interactions with cultured fibroblasts: relationship to mitogenic stimulation. Ann. N. Y. Acad. Sci. 485:240-248 (1986).
33. Bar-Shavit, R., A. Eldor, and I. Vlodavsky. Binding of thrombin to subendothelial extracellular matrix. Protection and expression of functional properties. J. Clin. Invest. 84:1096-1104 (1989).
34. Tapparelli, C., R. Metternich, and N. S. Cook. Structure and function of thrombin receptors. Structure and function of thrombin receptors. Trends Pharmacol. Sci. 14:426-428 (1993).
35. Tiruppathi C., H. Lum, T. T. Andersen, J. W. Fenton II, and A. B. Malik. Thrombin receptor 14-amino acid peptide binds to endothelial cells and stimulates calcium transients. Am. J. Physiol. 263:L595-L601 (1992).
36. Tadaka, M., O. Ito, M. Kogushi, H. Kobayashi, T. Yamada, H. Tanaka, S. Yoshitake, and I. Saito. Binding of biotinylated thrombin receptor peptide to cloned thrombin receptor overexpressed in baby hamster kidney cells. J. Recept. Signal Transduct. Res. 21:349-358 (1995).
37. Brass, L. F. Issues in the development of thrombin receptor antagonists. Thromb. Haemostasis. 74:499-505 (1996).
38. Norton, K. J., R. M. Scarborough, J. L. Kutok, M.-A. Escobedo, L. Nannizzi, and B. S. Coller. Immunologic analysis of the cloned platelet thrombin receptor activation mechanism: evidence supporting receptor cleavage, release of the N-terminal peptide, and insertion of the tethered ligand into a protected environment. Blood 82:2125-2136 (1993).
39. Brass, L. F., R. R. Vassallo, Jr., E. Belmonte, M. Ahuja, K. Cichowski, and J. A. Hoxie. Structure and function of the human platelet thrombin receptor. J. Biol. Chem. 267:13795-13798 (1992).