Determination of PAR4 numbers on the surface of human platelets: no effect of the single nucleotide polymorphism rs773902
Sign Up to like & getrecommendations! Published in 2020 at "Platelets"
DOI: 10.1080/09537104.2020.1810654
Abstract: Abstract The thrombin receptor, protease-activated receptor 4 (PAR4), is important for platelet activation and is the target of emerging anti-thrombotic drugs. A frequently occurring single nucleotide polymorphism (SNP; rs773902) causes a function-altering PAR4 sequence variant… read more here.
Keywords: par4; single nucleotide; par4 numbers; pharmacology ... See more keywords
New oral protease-activated receptor 4 antagonist BMS-986120: tolerability, pharmacokinetics, pharmacodynamics, and gene variant effects in humans
Sign Up to like & getrecommendations! Published in 2022 at "Platelets"
DOI: 10.1080/09537104.2022.2088719
Abstract: Abstract BMS-986120 is a novel first-in-class oral protease-activated receptor 4 (PAR4) antagonist exhibiting robust antithrombotic activity that has shown low bleeding risk in monkeys. We sought to assess pharmacokinetics, pharmacodynamics, and tolerability of BMS-986120 in… read more here.
Keywords: bms 986120; protease activated; par4; oral protease ... See more keywords
Downregulation of iNOS, IL-1β, and P2X7 Expression in Mast Cells via Activation of PAR4 Contributes to the Inhibition of Visceral Hyperalgesia in Rats
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DOI: 10.1155/2018/3256908
Abstract: Protease-activated receptor 4 (PAR4) is implicated in the inhibition of visceral hyperalgesia. In the present study, the effects of PAR4 activation on visceral hypersensitivity and expression of inflammatory mediators, including interleukin-1β (IL-1β), P2RX7 purinergic receptor… read more here.
Keywords: par4; inos p2x7; visceral hyperalgesia; expression ... See more keywords
Selective Inhibition of PAR4 (Protease-Activated Receptor 4)-Mediated Platelet Activation by a Synthetic Nonanticoagulant Heparin Analog
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DOI: 10.1161/atvbaha.118.311758
Abstract: Objective— PAR4 (protease-activated receptor 4), one of the thrombin receptors in human platelets, has emerged as a promising target for the treatment of arterial thrombotic disease. Previous studies implied that thrombin exosite II, known as… read more here.
Keywords: thrombin; activation; par4; heparin ... See more keywords
Abstract 16292: Selective Platelet Protease-Activated-Receptor (PAR)1 and PAR4 Mediated Thrombin Desensitisation in the Elderly is Correlated With Inflammation and Chronic Thrombin Receptor Stimulation
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DOI: 10.1161/circ.142.suppl_3.16292
Abstract: Introduction: Platelet activation, by adenosine diphosphate (ADP) via P2Y12 receptors and thrombin via PAR1 and PAR4, is a key therapeutic target in cardiovascular disease (CVD). The efficacy of an... read more here.
Keywords: par4; 16292 selective; receptor; selective platelet ... See more keywords
A function-blocking PAR4 antibody is markedly antithrombotic in the face of a hyperreactive PAR4 variant.
Sign Up to like & getrecommendations! Published in 2018 at "Blood advances"
DOI: 10.1182/bloodadvances.2017015552
Abstract: Thrombin activates human platelets via 2 protease-activated receptors (PARs), PAR1 and PAR4, both of which are antithrombotic drug targets: a PAR1 inhibitor is approved for clinical use, and a PAR4 inhibitor is in trial. However,… read more here.
Keywords: par4 variant; function blocking; par4; antibody ... See more keywords