Discovery of novel protease activated receptors 1 antagonists with potent antithrombotic activity in vivo

…, A Bocquet, F Nadal-Wollbold, D Cussac…

Index: Perez, Michel; Lamothe, Marie; Maraval, Catherine; Mirabel, Etienne; Loubat, Chantal; Planty, Bruno; Horn, Clemens; Michaux, Julien; Marrot, Sebastien; Letienne, Robert; Pignier, Christophe; Bocquet, Arnaud; Nadal-Wollbold, Florence; Cussac, Didier; De Vries, Luc; Le Grand, Bruno Journal of Medicinal Chemistry, 2009 , vol. 52, # 19 p. 5826 - 5836

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Citation Number: 36

Abstract

Protease activated receptors (PARs) or thrombin receptors constitute a class of G-protein- coupled receptors (GPCRs) implicated in the activation of many physiological mechanisms. Thus, thrombin activates many cell types such as vascular smooth muscle cells, leukocytes, endothelial cells, and platelets via activation of these receptors. In humans, thrombin- induced platelet aggregation is mediated by one subtype of these receptors, termed PAR1 ...