Protease-Activated Receptors (PAR)
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PAR-1 Antagonist
Vorapaxar (SCH 530348) is a potent and orally active thrombin receptor (PAR-1) antagonist with Ki of 8.1 nM.
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- Cansu Tekin, .et al. Macrophage-secreted MMP9 induces mesenchymal transition in pancreatic cancer cells via PAR1 activation, Cell Oncol (Dordr), 2020, Aug 18 PMID: 32809114
- Cansu Tekin, .et al. PAR1 signaling on tumor cells limits tumor growth by maintaining a mesenchymal phenotype in pancreatic cancer, Oncotarget, 2018, Aug 10; 9(62): 32010-32023 PMID: 30174793
- Claushuis TA, .et al. Thrombin contributes to protective immunity in pneumonia-derived sepsis via fibrin polymerization and platelet-neutrophil interactions, J Thromb Haemost, 2017, Apr;15(4):744-757 PMID: 28092405
- Maaike Waasdorp, .et al. Plasmin reduces fibronectin deposition by mesangial cells in a protease-activated receptor-1 independent manner, Biochem Biophys Rep, 2017, Jul; 10: 152-156 PMID: 29114573
- Joseph C. Mudd, .et al. Inflammatory Function of CX3CR1+ CD8+ T Cells in Treated HIV Infection Is Modulated by Platelet Interactions, J Infect Dis, 2016, Dec 15; 214(12): 1808-1816 PMID: 27703039
- Corey E. Tabit, .et al. Elevated Angiopoietin-2 Level in Patients With Continuous-Flow Left Ventricular Assist Devices Leads to Altered Angiogenesis and Is Associated With Higher Non-Surgical Bleeding, Circulation, 2016, Jul 12; 134(2): 141-152 PMID: 27354285
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PAR1 inhibitor
ML-161 is an inhibitor of protease-activated receptor 1 (PAR1)-mediated platelet activation (IC50 = 0.26 μM for the inhibition of platelet P-selectin expression on human platelets).
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