Combined blockade of thrombin anion binding exosite-1 and PAR4 produces synergistic antiplatelet effect in human platelets

• Published in: Thrombosis and haemostasis Vol. 105; no. 1; p. 88
• Main Authors: Wu, Chin-Chung, Wang, Wei-Ya, Wei, Chien-Kei, Teng, Che-Ming
• Format: Journal Article
• Language: English
• Published: Germany 01.01.2011
• Subjects: Blood Platelets - cytology; Blood Platelets - drug effects; Blood Platelets - physiology; Calcium Signaling - drug effects; Cells, Cultured; Drug Synergism; Drug Therapy, Combination; Hirudins - pharmacology; Humans; Indazoles - pharmacology; Peptide Fragments - pharmacology; Platelet Aggregation Inhibitors - therapeutic use; Prothrombin - antagonists & inhibitors; Receptors, Thrombin - antagonists & inhibitors
• ISSN: 0340-6245
• DOI: 10.1160/TH10-05-0305

Thrombin exosite-1 mediates the specific binding of thrombin with fibrinogen and protease-activated receptor (PAR) 1. Exosite-1 inhibitors have been shown to effectively decrease the clotting activity of thrombin, while their antiplatelet effects are relatively weak. In the present study, the inhibi...