Development of Potent Thrombin Receptor Antagonist Peptides

1996 ◽  
Vol 39 (25) ◽  
pp. 4879-4887 ◽  
Author(s):  
Michael S. Bernatowicz ◽  
Clifford E. Klimas ◽  
Karen S. Hartl ◽  
Marianne Peluso ◽  
Nick J. Allegretto ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Thrombin Receptor ◽  
Antagonist Peptides ◽  
Thrombin Receptor Antagonist

scholarly journals Thrombin-Receptor Antagonist Vorapaxar in Acute Coronary Syndromes

2012 ◽  
Vol 366 (1) ◽  
pp. 20-33 ◽  
Author(s):  
Pierluigi Tricoci ◽  
Zhen Huang ◽  
Claes Held ◽  
David J. Moliterno ◽  
Paul W. Armstrong ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Acute Coronary Syndromes ◽  
Thrombin Receptor ◽  
Coronary Syndromes ◽  
Thrombin Receptor Antagonist

Thrombin receptor-mediated vascular relaxation differentiated by a receptor antagonist and desensitization

1994 ◽  
Vol 267 (5) ◽  
pp. H1962-H1967 ◽  
Author(s):  
B. Tesfamariam
Keyword(s):  
Receptor Antagonist ◽  
Vascular Endothelium ◽  
Active Site ◽  
Thrombin Receptor ◽  
Vascular Relaxation ◽  
Low Concentrations ◽  
Heterologous Desensitization ◽  
Tethered Ligand ◽  
Pig Coronary Arteries ◽  
Thrombin Receptor Antagonist

The vasorelaxant actions of the serine protease, alpha-thrombin, are selectively blocked by the thrombin active site inhibitors, suggesting that proteolytic cleavage is required for alpha-thrombin-induced release of nitric oxide. Whether these relaxations are caused by interaction with a thrombin receptor was evaluated using a prototype thrombin receptor antagonist, a decapeptide analogue of the tethered ligand thrombin receptor [3-mercapto-propionyl-Phe-Cha-Cha-Arg-Lys-Pro-Asn-Asp-Lys-amide (c186–65)]. In rings of pig coronary arteries with endothelium contracted submaximally with U-46619, the relaxation caused by extremely low concentrations of alpha-thrombin were mimicked by the synthetic thrombin receptor-activating peptide (TRAP-7: SFLLRNP). These relaxations were inhibited by C186–65. In contrast, C186–65 had no effect on the relaxations caused by bradykinin and serotonin. Exposure of arteries to alpha-thrombin or TRAP-7 caused heterologous desensitization to subsequent stimulation by alpha-thrombin or TRAP-7 but not by bradykinin. These studies support the hypothesis that alpha-thrombin-induced endothelium-dependent relaxations occur by activation of the cloned “tethered-ligand” thrombin receptor in vascular endothelium.

ChemInform Abstract: Eryloside F, a Novel Penasterol Disaccharide Possessing Potent Thrombin Receptor Antagonist Activity.

ChemInform ◽  
2010 ◽  
Vol 31 (28) ◽  
pp. no-no
Author(s):  
Paul Stead ◽  
Steve Hiscox ◽  
Phil S. Robinson ◽  
Nicholas B. Pike ◽  
Philip J. Sidebottom ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Thrombin Receptor ◽  
Antagonist Activity ◽  
Thrombin Receptor Antagonist
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