Thrombin Receptor Structure and Function

Shaun R Coughlin

doi:10.1055/s-0038-1646186

Thrombosis and Haemostasis, Table of Contents

Thromb Haemost 1993; 70(01): 184-187
DOI: 10.1055/s-0038-1646186

State-of-the-Art Lecture

Vessel Wall Receptors

Schattauer GmbH Stuttgart

Thrombin Receptor Structure and Function

Shaun R Coughlin

Cardiovascular Research Institute, University of California, San Francisco, CA, USA

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Abstract

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References

References
1 Walz D, Fenton II JW, Shuman M. Bioregulatory functions of thrombin. Ann NY Acad Sci 1986; 485: 1-449
2 Davey M, Luscher E. Actions of thrombin and other coagulant and proteolytic enzymes on blood platelets. Nature 1967; 216: 857
3 Berndt M, Phillips D. Platelet membrane proteins: composition and receptor function. In: Platelets in Biology and Pathology. Gordon JL. (ed). Biomedical Press; Elsevier/North Holland: 1981. pp. 43-74
4 Eidt J, Allison P, Nobel S, Ashton J, Golino P, McNatt J, Buja L, Willerson J. Thrombin is an important mediator of platelet aggregation in stenosed canine coronary arteries with endothelial injury. J Clin Invest 1989; 84: 18-27
5 Hanson S, Harker L. Interruption of acute platelet-dependent thrombosis by the synthetic antithrombin PPACK. Proc Natl Acad Sci USA 1988; 85: 3184-3188
6 Fitzgerald D, Fitzgerald G. Role of thrombin and thromboxane A2 in reocclusion following coronary thrombolysis. Proc Natl Acad Sci USA 1989; 86: 7585-7589
7 Jang IK, Gold H, Ziskind A, Leinbach R, Fallon J, Collen D. Prevention of platelet-rich arterial thrombosis by selective thrombin inhibition. Circulation 1989; 81: 219-225
8 Heras M, Chesebro J, Penny W, Bailey K, Badimon L, Fuster V. Effects of thrombin inhibition on the development of acute platelet-thrombus deposition during angioplasty in pigs. Circulation 1989; 79: 657-665
9 Theroux P, Ouimet H, McCums J. Aspirin, heparin, or both to treat acute unstable angina. N Engl J Med 1989; 319: 1105-1111
10 Bar-Shavit R, Kahn A, Wilner G, Fenton II J. Monocyte chemotaxis: stimulation by specific exosite region in thrombin. Science 1983; 220: 728
11 Chen L, Teng N, Buchanan J. Mitogenicity of thrombin and surface alterations on mouse splenocytes. Exp Cell Res 1976; 101: 41-46
12 Chen L, Buchanan J. Mitogenic activity of blood components. I. Thrombin and prothrombin. Proc Natl Acad Sci USA 1975; 72: 131-135
13 McNamara C, Sarembok I, Gimple L, Fenton J, Coughlin S, Owens G. Thrombin stimulation of smooth muscle cell proliferation is mediated by a proteolytic, receptor-mediated mechanism. J Clin Invest 1992; 91: 94-98
14 Weksler B, Ley C, Jaffe E. Stimulation of endothelial cell prostacyclin production by thrombin, trypsin, and the ionophore A23187. J Clin Invest 1992; 62: 923-930
15 Prescott S, Zimmerman G, Mclntyre T. Human endothelial cells in culture produce platelet-activating factor when stimulated by thrombin. Proc Natl Acad Sci USA 1984; 81: 3534-3538
16 Gelehrter T, Sznycer-Laszyk R. Thrombin induction of plasminogen activator-inhibitor in cultured human endothelial cells. J Clin Invest 1986; 77: 165-169
17 Daniel T, Gibbs V, Milfay D, Garavoy M, Williams L. Thrombin stimulates c-sis gene expression in microvascular endothelial cells. J Biol Chem 1986; 261: 9579-9582
18 Zimmerman G, Mclntyre T, Prescott S. Thrombin stimulates neutrophil adherence by an endothelial cell-dependent mechanism. Ann NY Acad Sci 1986; 485: 349-368
19 Hattori R, Hamilton K, Fugate R, McEver R, Sims P. Stimulated secretion of endothelial vWF is accompanied by rapid redistribution to the cell surface of the intracellular granule membrane protein GMP-140. J Biol Chem 1989; 264: 7768-7771
20 Vu TK, Hung D, Wheaton V, Coughlin S. Molecular cloning of a functional thrombin receptor reveals a novel proteolytic mechanism of receptor activation. Cell 1991; 64: 1057-1068
21 Coughlin S, Vu TK, Hung D, Wheaton V. Perspectives. Characterization of the cloned platelet thrombin receptor: issues and opportunities. J Clin Invest 1992; 89: 351-355
22 Rydel T, Rabichandran K, Tulinsky A, Bode W, Huber R, Roitsch C, Fenton II J. The structure of a complex of recombinant hirudin and human alpha-thrombin. Science 1990; 249: 277-280
23 Hung D, Wong Y, Vu TK, Coughlin S. The cloned platelet thrombin receptor couples to at least two distinct effectors to stimulate both phosphoinositide hydrolysis and inhibit adenylyl cyclase. J Biol Chem 1992; 267: 20831-20834
24 Vu TK, Wheaton V, Hung D, Coughlin S. Domains specifying thrombin-receptor interaction. Nature 1991; 353: 674-677
25 Liu L, Vu TK, Esmon C, Coughlin S. The region of the thrombin receptor resembling hirudin binds to thrombin and alters enzyme specificity. J Biol Chem 1991; 266: 16977-16980
26 Hung D, Vu TK, Wheaton V, Charo I, Nelken N, Esmon N, Esmon C, Coughlin S. “Mirror image” antagonists of thrombin-induced platelet activation based on thrombin receptor structure. J Clin Invest 1992; 89: 444-450
27 Ishii K, Hein L, Kobilka B, Coughlin S. Kinetics of thrombin receptor cleavage on intact cells: relation to signalling. J Biol Chem 1993; 268: 9780-9786
28 Bode W, Schwager P, Huber R. The transition of bovine trypsinogen to a trypsin-like state upon strong ligand binding. J Mol Biol 1978; 118: 99-112
29 Vouret-Craviari V, Obberghen-Schilling V, Rasmussen U, Pavirani A, Lecocq J, Pouyssegur J. Synthetic α-thrombin receptor peptides activate G-protein coupled signalling pathways but are unable to induce mitogenesis. Mol Biol Cell 1992; 3: 95-102
30 Vassallo Jr. R, Kieber-Emmons T, Cichowski K, Brass L. Structure-function relationships in the activation of platelet thrombin receptors by receptor-derived peptides. J Biol Chem 1992; 267: 6081-6085
31 Scarborough R, Naughton M, Teng W, Hung D, Rose J, Vu TK, Wheaton V, Turck C, Coughlin S. Tethered ligand agonist peptides: structural requirements for thrombin receptor activation reveal mechanism of proteolytic unmasking of agonist function. J Biol Chem 1992; 267: 13146-13149
32 Coller B, Ward P, Ceruso M, Scudder L, Springer K, Kutok J, Prest-wich G. Thrombin receptor activating peptides: importance of the N-terminal serine and its ionization state as judged by pH dependence, NMR spectroscopy, and cleavage by aminopeptidase M. Biochemistry 1992; 31: 11713-11720
33 Detwiler T, Feinman R. Kinetics of the thrombin-induced release of calcium (II) by platelets. Biochemistry 1973; 12: 282-289
34 Martin B, Feinman R, Detwiler T. Platelet stimulation by thrombin and other proteases. Biochemistry 1975; 14: 1308-1314
35 Martin B, Wasiewski W, Fenton II J, Detwiler T. Equilibrium binding of thrombin to platelets. Biochemistry 1976; 15: 4886-4893
36 Rittenhouse-Simmons S. Production of diglyceride from phos-phatidylinositol in activated human platelets. J Clin Invest 1979; 63: 580-587
37 Paris S, Pouyssegur J. Pertussis toxin inhibits thrombin-induced activation of phosphoinositide hydrolysis and Na⁺/H⁺ exchange in hamster fibroblasts. EMBO J 1986; 5: 55-60
38 Dohlman H, Thorner J, Caron M, Lefkowitz R. Model systems for the study of seven transmembrane segment receptors. Ann Rev Biochem 1992; 60: 653-688
39 Brass L. Homologous desensitization of HEL cell thrombin receptors. J Biol Chem 1992; 267: 6044-6050
40 Huang R, Sorisky A, Church W, Simons E, Rittenhouse S. Thrombin receptor-directed ligand accounts for activation by thrombin of platelet phospholipase C and accumulation of 3-phosphorylated phosphoinositides. J Biol Chem 1991; 266: 18435-18438
41 Hung D, Vu TK, Wheaton V, Ishii K, Coughlin S. The cloned platelet thrombin receptor is necessary for thrombin-induced platelet activation. Blocking antiserum to the thrombin receptor's hirudin-like domain. J Clin Invest 1992; 89: 1350-135
42 Brass L, Vassallo R, Belmonte E, Ahuja M, Cichowski K, Hoxie J. Structure and function of the human platelet thrombin receptor. Studies using monoclonal antibodies directed against a defined domain within the receptor N terminus. J Biol Chem 1992; 267: 13795-13798
43 Nelken N, Soifer S, O'Keefe J, Vu TK, Charo I, Coughlin S. Thrombin receptor expression in normal and atherosclerotic human arteries. J Clin Invest 1992; 90: 1614-1621
44 Coughlin S. The platelet thrombin receptor. In: Molecular Biology of Thrombosis and Hemostasis. Roberts HR, High KA. (eds). Marcel Dekker, Inc.; New York: 1993. (in press)