Q94 is not a selective modulator of proteinase-activated receptor 1 (PAR1) in platelets

References

• Raskob GE. ISTH Steering Committee for World Thrombosis Day. Thrombosis: a major contributor to the global disease burden. J Thromb Haemost 2014;12:1580–1590.
   PubMed Web of Science ®Google Scholar
• Coughlin SR. Thrombin signalling and protease-activated receptors. Nature 2000;407:258–264. doi:10.1038/35025229.
   PubMed Web of Science ®Google Scholar
• Hamilton JR. Protease-activated receptors as targets for antiplatelet therapy. Blood Rev 2009;23:61–65. doi:10.1016/j.blre.2008.06.002.
   PubMed Web of Science ®Google Scholar
• Cunningham M, McIntosh K, Bushell T, Sloan G, Plevin R. Proteinase-activated receptors (PARs) as targets for antiplatelet therapy. Biochem Soc Trans 2016;44:606–612. doi:10.1042/BST20150282.
   PubMed Web of Science ®Google Scholar
• Willis Fox O, Preston RJS. Molecular basis of protease-activated receptor 1 signaling diversity. J Thromb Haemost 2020;18:6–16. doi:10.1111/jth.14643.
   PubMed Web of Science ®Google Scholar
• Sinha RK, Wang Y, Zhao Z, Xu X, Burnier L, Gupta N, Fernández JA, Martin G, Kupriyanov S, Mosnier LO, et al. PAR1 biased signaling is required for activated protein C in vivo benefits in sepsis and stroke. Blood 2018;131:1163–1171. doi:10.1182/blood-2017-10-810895.
   PubMed Web of Science ®Google Scholar
• Schuepbach RA, Feistritzer C, Fernández JA, Griffin JH, Riewald M. Protection of vascular barrier integrity by activated protein C in murine models depends on protease-activated receptor-1. Thromb Haemost 2009;101:724–733. doi:10.1160/TH08-10-0632.
   PubMed Web of Science ®Google Scholar
• Soh UJK, Trejo JA. Activated protein C promotes protease-activated receptor-1 cytoprotective signaling through β-arrestin and dishevelled-2 scaffolds. Proc Natl Acad Sci U S A 2011;108:E1372–E1380. doi:10.1073/pnas.1112482108.
   PubMedGoogle Scholar
• Magnani G, Bonaca MP, Braunwald E, Dalby AJ, Fox KAA, Murphy SA, Nicolau JC, Oude Ophuis T, Scirica BM, Spinar J, et al. Efficacy and safety of vorapaxar as approved for clinical use in the United States. J Am Heart Assoc 2015;4:e001505. doi:10.1161/JAHA.114.001505.
   PubMed Web of Science ®Google Scholar
• Flaumenhaft R, De Ceunynck K. Targeting PAR1: now what? Trends Pharmacol Sci 2017;38:701–716. doi:10.1016/j.tips.2017.05.001.
   PubMed Web of Science ®Google Scholar
• Bokoch MP, Jo H, Valcourt JR, Srinivasan Y, Pan AC, Capponi S, Grabe M, Dror RO, Shaw DE, DeGrado WF, et al. Entry from the lipid bilayer: a possible pathway for inhibition of a peptide G protein-coupled receptor by a lipophilic small molecule. Biochemistry 2018;57:5748–5758. doi:10.1021/acs.biochem.8b00577.
   PubMed Web of Science ®Google Scholar
• Aisiku O, Peters CG, De Ceunynck K, Ghosh CC, Dilks JR, Fustolo-Gunnink SF, Huang M, Dockendorff C, Parikh SM, Flaumenhaft R, et al. Parmodulins inhibit thrombus formation without inducing endothelial injury caused by vorapaxar. Blood 2015;125:1976–1985. doi:10.1182/blood-2014-09-599910.
   PubMed Web of Science ®Google Scholar
• Dowal L, Sim DS, Dilks JR, Blair P, Beaudry S, Denker BM, Koukos G, Kuliopulos A, Flaumenhaft R. Identification of an antithrombotic allosteric modulator that acts through helix 8 of PAR1. Proc Natl Acad Sci U S A 2011;108:2951–2956. doi:10.1073/pnas.1014863108.
   PubMed Web of Science ®Google Scholar
• Gandhi DM, Majewski MW, Rosas R, Kentala K, Foster TJ, Greve E, Dockendorff C. Characterization of protease-activated receptor (PAR) ligands: parmodulins are reversible allosteric inhibitors of PAR1-driven calcium mobilization in endothelial cells. Bioorganic Med Chem 2018;26:2514–2529. doi:10.1016/j.bmc.2018.04.016.
   PubMed Web of Science ®Google Scholar
• De Ceunynck K, Peters CG, Jain A, Higgins SJ, Aisiku O, Fitch-Tewfik JL, Chaudhry SA, Dockendorff C, Parikh SM, Ingber DE, et al. PAR1 agonists stimulate APC-like endothelial cytoprotection and confer resistance to thromboinflammatory injury. Proc Natl Acad Sci U S A 2018;115:E982–E991. doi:10.1073/pnas.1718600115.
   PubMed Web of Science ®Google Scholar
• Deng X, Mercer PF, Scotton CJ, Gilchrist A, Chambers RC. Thrombin induces fibroblast CCL2/JE production and release via coupling of PAR1 to Gαq and cooperation between ERK1/2 and Rho kinase signaling pathways. Mol Biol Cell 2008;19:2520–2533. doi:10.1091/mbc.e07-07-0720.
   PubMed Web of Science ®Google Scholar
• Mercer PF, Johns RH, Scotton CJ, Krupiczojc MA, Königshoff M, Howell DCJ, McAnulty RJ, Das A, Thorley AJ, Tetley TD, et al. Pulmonary epithelium is a prominent source of proteinase-activated receptor-1-inducible CCL2 in pulmonary Fibrosis. Am J Respir Crit Care Med 2009;179:414–425. doi:10.1164/rccm.200712-1827OC.
   PubMed Web of Science ®Google Scholar
• Asteriti S, Daniele S, Porchia F, Dell’Anno MT, Fazzini A, Pugliesi I, Trincavelli ML, Taliani S, Martini C, Mazzoni MR, et al. Modulation of PAR1 signalling by benzimidazole compounds. Br J Pharmacol 2012;167:80–94. doi:10.1111/j.1476-5381.2012.01974.x.
   PubMed Web of Science ®Google Scholar
• Guan Y, Nakano D, Zhang Y, Li L, Liu W, Nishida M, Kuwabara T, Morishita A, Hitomi H, Mori K, et al. A protease-activated receptor-1 antagonist protects against podocyte injury in a mouse model of nephropathy. J Pharmacol Sci 2017;135:81–88. doi:10.1016/j.jphs.2017.09.002.
   Web of Science ®Google Scholar
• Scotton CJ, Krupiczojc MA, Königshoff M, Mercer PF, Lee YCG, Kaminski N, Morser J, Post JM, Maher TM, Nicholson AG, et al. Increased local expression of coagulation factor X contributes to the fibrotic response in human and murine lung injury. J Clin Invest 2009;119:2550–2563. doi:10.1172/JCI33288.
   PubMed Web of Science ®Google Scholar
• Millington-Burgess SL, Harper MT. Epigallocatechin gallate inhibits release of extracellular vesicles from platelets without inhibiting phosphatidylserine exposure. Sci Rep 2021;11. doi:10.1038/s41598-021-97212-8.
   PubMed Web of Science ®Google Scholar
• Millington-Burgess SL, Bonna AM, Rahman T, Harper MT. Ethaninidothioic acid (R5421) is not a selective inhibitor of platelet phospholipid scramblase activity. Br J Pharmacol 2020;177:4007–4020. doi:10.1111/bph.15152.
   PubMed Web of Science ®Google Scholar
• Davies JE, Lopresto D, Apta BHR, Lin Z, Ma W, Harper MT. Using Yoda-1 to mimic laminar flow in vitro: a tool to simplify drug testing. Biochem Pharmacol 2019;168:473–480. doi:10.1016/j.bcp.2019.08.013.
   PubMed Web of Science ®Google Scholar
• Knight E. The Development of Novel Vorapaxar Analogues as Topical Protease Activated Receptor-1 Antagonists for the Treatment of Idiopathic Pulmonary Fibrosis. [Dr. thesis]. London: UCL (University Coll); 2016.
   Google Scholar