PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 19882073-0 2009 Improving antiplatelet therapy for atherothrombotic disease: preclinical results with SCH 530348, the first oral thrombin receptor antagonist selective for PAR-1. vorapaxar 86-96 coagulation factor II, thrombin Homo sapiens 113-121 20307225-0 2010 Thrombin receptor antagonism -the potential of antiplatelet medication SCH 530348. vorapaxar 71-81 coagulation factor II, thrombin Homo sapiens 0-8 20307225-12 2010 TAKE HOME MESSAGE: SCH 530348 is a new, orally administered antiplatelet agent that blocks the protease-activated thrombin receptor on the platelet. vorapaxar 19-29 coagulation factor II, thrombin Homo sapiens 114-122 19699853-1 2009 BACKGROUND: The protease-activated receptor 1 (PAR-1), the main platelet receptor for thrombin, represents a novel target for treatment of arterial thrombosis, and SCH 530348 is an orally active, selective, competitive PAR-1 antagonist. vorapaxar 164-174 coagulation factor II, thrombin Homo sapiens 86-94 19699854-2 2009 SCH 530348 is a novel antiplatelet agent that selectively inhibits the cellular actions of thrombin via antagonism of the protease-activated receptor 1. vorapaxar 0-10 coagulation factor II, thrombin Homo sapiens 91-99 19705342-0 2009 SCH-530348, a thrombin receptor (PAR-1) antagonist for the prevention and treatment of atherothrombosis. vorapaxar 0-10 coagulation factor II, thrombin Homo sapiens 14-22 19715408-0 2009 SCH 530348: a novel oral thrombin receptor antagonist. vorapaxar 0-10 coagulation factor II, thrombin Homo sapiens 25-33 19715408-1 2009 SCH 530348, a synthetic tricyclic 3-phenylpyridine, is an orally active fourth generation himbacine-based antagonist of the protease-activated receptor (PAR)-1, the primary receptor for thrombin on platelets in humans. vorapaxar 0-10 coagulation factor II, thrombin Homo sapiens 186-194 19715408-2 2009 SCH 530348 is the first in a new class of compounds that inhibit thrombin-mediated platelet aggregation without affecting the enzymatic activity of thrombin on fibrinogen. vorapaxar 0-10 coagulation factor II, thrombin Homo sapiens 65-73 20836572-0 2010 Thrombin receptor antagonists for the treatment of atherothrombosis: therapeutic potential of vorapaxar and E-5555. vorapaxar 94-103 coagulation factor II, thrombin Homo sapiens 0-8 19882073-3 2009 SCH 530348, a potent thrombin receptor antagonist (TRA) selective for PAR-1, has been evaluated in preclinical studies, demonstrating complete and sustained inhibition of thrombin/TRAP-induced platelet aggregation without a concomitant increase in the risk of bleeding. vorapaxar 0-10 coagulation factor II, thrombin Homo sapiens 21-29 19882073-3 2009 SCH 530348, a potent thrombin receptor antagonist (TRA) selective for PAR-1, has been evaluated in preclinical studies, demonstrating complete and sustained inhibition of thrombin/TRAP-induced platelet aggregation without a concomitant increase in the risk of bleeding. vorapaxar 0-10 coagulation factor II, thrombin Homo sapiens 171-179 33776786-5 2021 Thrombin-induced TF was also inhibited by a PAR1 antagonist, Vorapaxar. vorapaxar 61-70 coagulation factor II, thrombin Homo sapiens 0-8 18574020-12 2008 A new oral antiplatelet thrombin-receptor antagonist, TRA-SCH 530348, is in early clinical trials. vorapaxar 58-68 coagulation factor II, thrombin Homo sapiens 24-32 34944024-9 2021 Thrombin-induced uptake of oxLDL was augmented by additional TLR2/4 stimulation and abrogated by vorapaxar. vorapaxar 97-106 coagulation factor II, thrombin Homo sapiens 0-8 34718032-5 2021 Vorapaxar is a novel antiplatelet therapy that inhibits thrombin-mediated platelet aggregation to prevent recurrence of ischemic events. vorapaxar 0-9 coagulation factor II, thrombin Homo sapiens 56-64 35006035-5 2022 One such medical therapy, vorapaxar, is a potent inhibitor of protease activated receptor-1 which mediates the cellular effects of thrombin. vorapaxar 26-35 coagulation factor II, thrombin Homo sapiens 131-139 33609100-1 2019 BACKGROUND: Vorapaxar inhibits the thrombin-mediated activation of platelets, reduces thrombotic events in patients with myocardial infarction or peripheral arterial disease while increasing bleeding. vorapaxar 12-21 coagulation factor II, thrombin Homo sapiens 35-43 32308016-1 2020 Vorapaxar specifically and effectively inhibits protease activated receptor-1 and may reduce thrombin-mediated ischemic events without interfering primary hemostasis. vorapaxar 0-9 coagulation factor II, thrombin Homo sapiens 93-101 31642690-1 2019 BACKGROUND: Vorapaxar inhibits the thrombin-mediated activation of platelets, reduces thrombotic events in patients with myocardial infarction or peripheral arterial disease while increasing bleeding. vorapaxar 12-21 coagulation factor II, thrombin Homo sapiens 35-43 33078834-8 2020 These beneficial effects were recapitulated in cultured tubular epithelial cells in which vorapaxar ameliorated thrombin- and hypoxia-induced TGF-beta expression and ECM accumulation. vorapaxar 90-99 coagulation factor II, thrombin Homo sapiens 112-120 28403576-1 2018 Vorapaxar is a first-in-class antagonist of the protease-activated receptor-1, the primary thrombin receptor on human platelets, which mediates the downstream effects of thrombin in hemostasis and thrombosis. vorapaxar 0-9 coagulation factor II, thrombin Homo sapiens 91-99 30324870-5 2019 Moreover, vorapaxar allows the inhibition of platelet activation by thrombin via protease-activated receptor-1 and has been approved for the use in patients with PAD and in those with a history of myocardial infarction. vorapaxar 10-19 coagulation factor II, thrombin Homo sapiens 68-76 30498684-5 2018 Oral platelet P2Y12 receptor inhibitors with enhanced potency, such as prasugrel and ticagrelor, as well as antiplatelet therapies such as vorapaxar inhibiting the thrombin-mediated platelet signaling pathway, constitute treatment opportunities for patients with DM and have shown to be associated with a greater reduction in ischemic recurrences, albeit at the cost of more bleeding. vorapaxar 139-148 coagulation factor II, thrombin Homo sapiens 164-172 29864779-4 2018 Vorapaxar dosing was guided by thrombin receptor-activating peptide-6-induced whole blood aggregometry. vorapaxar 0-9 coagulation factor II, thrombin Homo sapiens 31-39 29864779-6 2018 Vorapaxar significantly reduced the LPS-induced increase in pro-thrombin fragments F1 + 2 by a median of 27% (quartiles: 11-49%), thrombin-anti-thrombin concentrations by 22% (-3 to 46%) and plasmin-anti-plasmin levels by 38% (23-53%). vorapaxar 0-9 coagulation factor II, thrombin Homo sapiens 64-72 28403576-1 2018 Vorapaxar is a first-in-class antagonist of the protease-activated receptor-1, the primary thrombin receptor on human platelets, which mediates the downstream effects of thrombin in hemostasis and thrombosis. vorapaxar 0-9 coagulation factor II, thrombin Homo sapiens 170-178 28981200-9 2017 PAR-1 signaling through Galphaq was not required because vorapaxar blocked thrombin-induced calcium mobilization but had no effect on the ability of thrombin to impair GPVI-signaling. vorapaxar 57-66 coagulation factor II, thrombin Homo sapiens 75-83 28565918-0 2018 Role for Thrombin Receptor Antagonism With Vorapaxar in Secondary Prevention of Atherothrombotic Events: From Bench to Bedside. vorapaxar 43-52 coagulation factor II, thrombin Homo sapiens 9-17 28148395-12 2017 Thrombin induced dose-dependent EOC cell line proliferation was completely reversed by the PAR-1 antagonist vorapaxar. vorapaxar 108-117 coagulation factor II, thrombin Homo sapiens 0-8 27261371-11 2016 In addition, thrombin and MMP-1 induced VEGF in HRMEC and vorapaxar, a PAR1 inhibitor, inhibited thrombin-induced migration in HRMEC. vorapaxar 58-67 coagulation factor II, thrombin Homo sapiens 13-21 28063023-9 2017 However, the Thrombin-Receptor Antagonist in Secondary Prevention of Atherothrombotic Ischemic Events (TRA 2 P-TIMI 50) trial examined a more traditional composite endpoint and found a significant benefit with vorapaxar. vorapaxar 210-219 coagulation factor II, thrombin Homo sapiens 13-21 28135897-4 2017 Expert opinion: Vorapaxar inhibits platelet aggregation mediated by thrombin. vorapaxar 16-25 coagulation factor II, thrombin Homo sapiens 68-76 27489245-6 2017 Vorapaxar is a novel antiplatelet agent that targets the platelet protease-activated receptor 1 and inhibits thrombin-induced platelet activation. vorapaxar 0-9 coagulation factor II, thrombin Homo sapiens 109-117 27489245-8 2017 New data from the Thrombin-Receptor Antagonist in Secondary Prevention of Atherothrombotic Ischemic Events (TRA 2 P)-TIMI 50 trial MI cohort demonstrate that the subgroup of patients with T2DM exhibits increased benefit from vorapaxar use compared with non-T2DM patients. vorapaxar 225-234 coagulation factor II, thrombin Homo sapiens 18-26 27261371-11 2016 In addition, thrombin and MMP-1 induced VEGF in HRMEC and vorapaxar, a PAR1 inhibitor, inhibited thrombin-induced migration in HRMEC. vorapaxar 58-67 coagulation factor II, thrombin Homo sapiens 97-105 26386102-3 2015 Vorapaxar competitively inhibits thrombin from activating the receptor, thereby decreasing platelet aggregation. vorapaxar 0-9 coagulation factor II, thrombin Homo sapiens 33-41 26966273-5 2016 Pretreatment with the PAR1 antagonist vorapaxar caused lower residual alpha-thrombin responses in Y157C platelets than in controls, indicating greater platelet inhibition. vorapaxar 38-47 coagulation factor II, thrombin Homo sapiens 76-84 26984587-6 2016 The development of antiplatelet therapies associated with more potent oral platelet P2Y12receptor inhibition, including prasugrel and ticagrelor, as well as platelet inhibitors blocking alternative pathways, such as thrombin-mediated platelet inhibition with vorapaxar, may represent potential treatment options in DM patients. vorapaxar 259-268 coagulation factor II, thrombin Homo sapiens 216-224 27398626-3 2016 Vorapaxar is a first-in-class, novel antiplatelet agent that acts by antagonizing the PAR-1 receptor, inhibiting thrombin-mediated platelet activation. vorapaxar 0-9 coagulation factor II, thrombin Homo sapiens 113-121 27366081-2 2016 Vorapaxar is a tricyclic himbacine-derived reversible inhibitor of platelet surface protease activator receptor-1, which prevents thrombin from activating platelets. vorapaxar 0-9 coagulation factor II, thrombin Homo sapiens 130-138 27131284-6 2016 RESULTS: Vorapaxar abolished 67 of the 69 transcripts altered by more than twofold on addition of thrombin to HUVECs. vorapaxar 9-18 coagulation factor II, thrombin Homo sapiens 98-106 27131284-8 2016 Inflammatory gene expression after stimulation of thrombin generation was concentration-dependently suppressed by vorapaxar, dabigatran, and rivaroxaban. vorapaxar 114-123 coagulation factor II, thrombin Homo sapiens 50-58 26338971-3 2015 METHODS AND RESULTS: The Thrombin Receptor Antagonist in Secondary Prevention of Atherothrombotic Ischemic Events-Thrombolysis in Myocardial Infarction 50 (TRA 2 P-TIMI 50) was a randomized, double-blind, placebo-controlled trial of vorapaxar in 26,449 patients with previous atherothrombosis. vorapaxar 233-242 coagulation factor II, thrombin Homo sapiens 25-33 26022529-0 2015 In vitro pharmacological characterization of vorapaxar, a novel platelet thrombin receptor antagonist. vorapaxar 45-54 coagulation factor II, thrombin Homo sapiens 73-81 26022529-8 2015 Vorapaxar and M20 completely blocked thrombin-stimulated PAR1/beta-arrestin association in recombinant cells and abolished thrombin-stimulated calcium influx in washed human platelets and vascular smooth muscle cells. vorapaxar 0-9 coagulation factor II, thrombin Homo sapiens 37-45 26022529-8 2015 Vorapaxar and M20 completely blocked thrombin-stimulated PAR1/beta-arrestin association in recombinant cells and abolished thrombin-stimulated calcium influx in washed human platelets and vascular smooth muscle cells. vorapaxar 0-9 coagulation factor II, thrombin Homo sapiens 123-131 26022529-11 2015 In conclusion, vorapaxar is a potent PAR1 antagonist exhibiting saturable, reversible, selective binding with slow off-rate kinetics and effectively inhibits thrombin"s PAR1-mediated actions on human platelets. vorapaxar 15-24 coagulation factor II, thrombin Homo sapiens 158-166 26406386-0 2015 Platelet thrombin receptor antagonism with vorapaxar: pharmacology and clinical trial development. vorapaxar 43-52 coagulation factor II, thrombin Homo sapiens 9-17 25895464-1 2015 Vorapaxar (Zontivity ) is a first-in-class, potent and orally-active protease-activated receptor 1 (PAR-1) antagonist that blocks thrombin-mediated platelet activation without interfering with thrombin-mediated fibrin deposition. vorapaxar 0-9 coagulation factor II, thrombin Homo sapiens 130-138 24676931-4 2014 Vorapaxar is a novel, oral, protease-activated receptor-1 antagonist that inhibits thrombin-induced platelet activation. vorapaxar 0-9 coagulation factor II, thrombin Homo sapiens 83-91 24750101-9 2015 Vorapaxar treatment significantly inhibited thrombin-induced calcium mobilisation, leaving a residual, delayed response. vorapaxar 0-9 coagulation factor II, thrombin Homo sapiens 44-52 24750101-12 2015 In conclusion vorapaxar selectively antagonises the PAR1-mediated component of thrombin-induced platelet activation, leaving the PAR4-mediated response intact, which may explain why vorapaxar is well tolerated in patients undergoing CABG surgery since higher thrombin levels in this setting may override the effects of PAR1 antagonism through PAR4 activation, thus preserving haemostasis. vorapaxar 14-23 coagulation factor II, thrombin Homo sapiens 79-87 24750101-12 2015 In conclusion vorapaxar selectively antagonises the PAR1-mediated component of thrombin-induced platelet activation, leaving the PAR4-mediated response intact, which may explain why vorapaxar is well tolerated in patients undergoing CABG surgery since higher thrombin levels in this setting may override the effects of PAR1 antagonism through PAR4 activation, thus preserving haemostasis. vorapaxar 182-191 coagulation factor II, thrombin Homo sapiens 79-87 25525635-1 2014 Vorapaxar is a novel platelet inhibitor that potently and selectively inhibits thrombin-mediated platelet activation without interfering with thrombin-mediated cleavage of fibrinogen via antagonism of the platelet proteinase-activated receptor PAR1. vorapaxar 0-9 coagulation factor II, thrombin Homo sapiens 79-87 21248619-6 2012 This review provides an outline of the current status of understanding on platelet thrombin-receptor antagonist SCH 530348, focusing on its pharmacologic properties and clinical development. vorapaxar 112-122 coagulation factor II, thrombin Homo sapiens 83-91 26104312-6 2014 Vorapaxar, a thrombin receptor antagonist acts by reversible inhibition of the protease-activated receptor-1 (PAR-1). vorapaxar 0-9 coagulation factor II, thrombin Homo sapiens 13-21 23501976-1 2013 BACKGROUND: Vorapaxar is a novel antagonist of protease-activated receptor-1, the primary receptor for thrombin on human platelets that is also present on vascular endothelium and smooth muscle. vorapaxar 12-21 coagulation factor II, thrombin Homo sapiens 103-111 23396280-1 2013 BACKGROUND AND PURPOSE: Vorapaxar is an antiplatelet agent that antagonizes thrombin-mediated activation of the protease-activated receptor-1 on platelets. vorapaxar 24-33 coagulation factor II, thrombin Homo sapiens 76-84 27121783-0 2013 Effect of Food, Antacid, and Age on the Pharmacokinetics of the Oral Thrombin Receptor Antagonist Vorapaxar (SCH 530348) in Healthy Volunteers. vorapaxar 98-107 coagulation factor II, thrombin Homo sapiens 69-77 27121783-0 2013 Effect of Food, Antacid, and Age on the Pharmacokinetics of the Oral Thrombin Receptor Antagonist Vorapaxar (SCH 530348) in Healthy Volunteers. vorapaxar 109-119 coagulation factor II, thrombin Homo sapiens 69-77 22932716-1 2012 BACKGROUND: Vorapaxar inhibits platelet activation by antagonising thrombin-mediated activation of the protease-activated receptor 1 on human platelets. vorapaxar 12-21 coagulation factor II, thrombin Homo sapiens 67-75 22476387-1 2012 PURPOSE: Vorapaxar is an orally active protease-activated receptor 1 (PAR-1) antagonist that inhibits thrombin-induced platelet aggregation. vorapaxar 9-18 coagulation factor II, thrombin Homo sapiens 102-110 22443427-2 2012 Vorapaxar is a novel antiplatelet agent that selectively inhibits the cellular actions of thrombin through antagonism of PAR-1. vorapaxar 0-9 coagulation factor II, thrombin Homo sapiens 90-98 22077816-0 2012 Thrombin-receptor antagonist vorapaxar in acute coronary syndromes. vorapaxar 29-38 coagulation factor II, thrombin Homo sapiens 0-8 22077816-1 2012 BACKGROUND: Vorapaxar is a new oral protease-activated-receptor 1 (PAR-1) antagonist that inhibits thrombin-induced platelet activation. vorapaxar 12-21 coagulation factor II, thrombin Homo sapiens 99-107