2025

Cheng, N., Ramirez, M. G., Edwards, C., & Trejo, J. (2025). USP34 regulates endothelial PAR1 mRNA transcript expression and cellular signaling. Molecular Biology of the Cell, 36(2), ar12.
https://www.molbiolcell.org/doi/full/10.1091/mbc.E24-07-0294

2024

Park, S. H., Heo, Y., Kwon, I., Jo, S., Jeon, H., Lee, Y., ... & Namkung, W. (2024). Gestodene, a novel positive allosteric modulator of PAR1, enhances PAR1-mediated human platelet aggregation. Frontiers in Pharmacology, 15, 1430548.
https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2024.1430548/full

Tripathy, S., Singh, S., Banerjee, M., Modi, D. R., & Prakash, A. (2024). Coagulation proteases and neurotransmitters in pathogenicity of glioblastoma multiforme. International Journal of Neuroscience, 134(4), 398-408.
https://www.mdpi.com/1422-0067/25/18/10136

2023

Deng, L., Costa, F., Blake, K. J., Choi, S., Chandrabalan, A., Yousuf, M. S., ... & Chiu, I. M. (2023). S. aureus drives itch and scratch-induced skin damage through a V8 protease–PAR1 axis. Cell, 186(24), 5375-5393.
https://www.cell.com/cell/fulltext/S0092-8674%2823%2901164-9

Birch, C. A., Wedegaertner, H., Orduña-Castillo, L. B., Gonzalez Ramirez, M. L., Qin, H., & Trejo, J. (2023). Endothelial APC/PAR1 distinctly regulates cytokine-induced pro-inflammatory VCAM-1 expression. Frontiers in Molecular Biosciences, 10, 1211597.
https://www.frontiersin.org/journals/molecular-biosciences/articles/10.3389/fmolb.2023.1211597/full

Birch, C., Wedegaertner, H., & Orduña-Castillo, L. (2023). Endothelial APC/PAR1 distinctly regulates cytokine-induced pro-inflammatory VCAM-1.
https://pdfs.semanticscholar.org/258b/ae8d015771d161aebe21144807b8047cda78.pdf

Lok, S. W., Yiu, W. H., Zou, Y., Xue, R., Li, H., Ma, J., ... & Tang, S. C. (2023). Tubulovascular protection from protease-activated receptor-1 depletion during AKI-to-CKD transition. Nephrology Dialysis Transplantation, 38(10), 2232-2247.
https://academic.oup.com/ndt/article/38/10/2232/7076887

Regenauer, R. (2023). Der Einfluss von Rivaroxaban auf die Entstehung von arteriellen Thrombosen (Doctoral dissertation, LMU).
https://edoc.ub.uni-muenchen.de/32311/1/Regenauer_Ron.pdf

2022

Cao, D., Strainic, M. G., Counihan, D., Sridar, S., An, F., Hussain, W., ... & Medof, M. E. (2022). Vascular endothelial cells produce coagulation factors that control their growth via joint protease-activated receptor and C5a receptor 1 (CD88) signaling. The American Journal of Pathology, 192(2), 361-378.
https://www.sciencedirect.com/science/article/pii/S0002944021005101

Heo, Y., Jeon, H., & Namkung, W. (2022). PAR4-mediated PI3K/Akt and RhoA/ROCK signaling pathways are essential for thrombin-induced morphological changes in MEG-01 cells. International Journal of Molecular Sciences, 23(2), 776.
https://www.mdpi.com/1422-0067/23/2/776

Joseph, C., Berghausen, E. M., Behringer, A., Rauch, B., Ten Freyhaus, H., Gnatzy-Feik, L. L., ... & Rosenkranz, S. (2022). Coagulation-independent effects of thrombin and Factor Xa: role of protease-activated receptors in pulmonary hypertension. Cardiovascular Research, 118(16), 3225-3238.
https://academic.oup.com/cardiovascres/article/118/16/3225/6519149

McKelvey, M. C., Abladey, A. A., Small, D. M., Doherty, D. F., Williams, R., Scott, A., ... & Weldon, S. (2022). Cathepsin S contributes to lung inflammation in acute respiratory distress syndrome. American Journal of Respiratory and Critical Care Medicine, 205(7), 769-782.
https://www.atsjournals.org/doi/full/10.1164/rccm.202107-1631OC

Molinar-Inglis, O., Wozniak, J. M., Grimsey, N. J., Orduña-Castillo, L. B., Cheng, N., Lin, Y., ... & Trejo, J. (2022). Phosphoproteomic analysis of thrombin- and p38 MAPK-regulated signaling networks in endothelial cells. Journal of Biological Chemistry, 298(4).
https://www.jbc.org/article/S0021-9258(22)00241-1/fulltext

2021

Papadaki, S., Sidiropoulou, S., Moschonas, I. C., & Tselepis, A. D. (2021). Factor Xa and thrombin induce endothelial progenitor cell activation. The effect of direct oral anticoagulants. Platelets, 32(6), 807-814.
https://www.tandfonline.com/doi/abs/10.1080/09537104.2020.1802413

Han, X., de la Fuente, M., & Nieman, M. T. (2021). Complement factor C4a does not activate protease‐activated receptor 1 (PAR1) or PAR4 on human platelets. Research and Practice in Thrombosis and Haemostasis, 5(1), 104-110.
https://www.sciencedirect.com/science/article/pii/S2475037922013103

Molinar-Inglis, O., Birch, C. A., Nicholas, D., Orduña-Castillo, L., Cisneros-Aguirre, M., Patwardhan, A., ... & Trejo, J. (2021). aPC/PAR1 confers endothelial anti-apoptotic activity via a discrete, β-arrestin-2–mediated SphK1–S1PR1–Akt signaling axis. Proceedings of the National Academy of Sciences, 118(49), e2106623118.
https://www.pnas.org/doi/full/10.1073/pnas.2106623118

Arakaki, A. K., Pan, W. A., Wedegaertner, H., Roca-Mercado, I., Chinn, L., Gujral, T. S., & Trejo, J. (2021). α-Arrestin ARRDC3 tumor suppressor function is linked to GPCR-induced TAZ activation and breast cancer metastasis. Journal of Cell Science, 134(8).
https://journals.biologists.com/jcs/article/134/8/jcs254888/237789

Ivanov, I. (2021). Role of Monocytes and Neutrophils in Thrombosis (Doctoral dissertation).
https://www.repository.cam.ac.uk/items/fabd15d2-33e7-4b5c-b509-a793315d8a86

Bukowska, A., Schild, L., Bornfleth, P., Peter, D., Wiese-Rischke, C., Gardemann, A., ... & Goette, A. (2020). Activated clotting factor X mediates mitochondrial alterations and inflammatory responses via protease-activated receptor signaling in alveolar epithelial cells. European Journal of Pharmacology, 869, 172875.
https://www.sciencedirect.com/science/article/pii/S0014299919308271
* Vorapaxar and GB83 from Axon

Peng, S., Grace, M. S., Gondin, A. B., Retamal, J. S., Dill, L., Darby, W., ... & McIntyre, P. (2020). The transient receptor potential vanilloid 4 (TRPV4) ion channel mediates protease activated receptor 1 (PAR1)-induced vascular hyperpermeability. Laboratory Investigation, 100(8), 1057-1067.
https://www.nature.com/articles/s41374-020-0430-7

Price, R., Ferrari, E., Gardoni, F., Mercuri, N. B., & Ledonne, A. (2020). Protease-activated receptor 1 (PAR1) inhibits synaptic NMDARs in mouse nigral dopaminergic neurons. Pharmacological Research, 160, 105185.
https://www.sciencedirect.com/science/article/pii/S1043661820314936
* Vorapaxar/SCH530348 and E5555 from Axon

2020

Bukowska, A., Schild, L., Bornfleth, P., Peter, D., Wiese-Rischke, C., Gardemann, A., ... & Goette, A. (2020). Activated clotting factor X mediates mitochondrial alterations and inflammatory responses via protease-activated receptor signaling in alveolar epithelial cells. European Journal of Pharmacology, 869, 172875.
https://www.sciencedirect.com/science/article/pii/S0014299919308271

Byskov, K., Le Gall, S. M., Thiede, B., Camerer, E., & Kanse, S. M. (2020). Protease activated receptors (PAR)-1 and -2 mediate cellular effects of factor VII activating protease (FSAP). The FASEB Journal, 34(1), 1079-1090.
https://onlinelibrary.wiley.com/doi/abs/10.1096/fj.201801986RR

Schanoski, A. S., Le, T. T., Kaiserman, D., Rowe, C., Prow, N. A., Barboza, D. D., ... & Muller, D. (2020). Granzyme A in Chikungunya and Other Arboviral Infections. Frontiers in Immunology, 10, 3083.
https://www.frontiersin.org/articles/10.3389/fimmu.2019.03083/full

2019

Bozzelli, P. L., Yin, T., Avdoshina, V., Mocchetti, I., Conant, K. E., & Maguire-Zeiss, K. A. (2019). HIV-1 Tat promotes astrocytic release of CCL2 through MMP/PAR-1 signaling. Glia, 67(9), 1719-1729.
https://onlinelibrary.wiley.com/doi/abs/10.1002/glia.23642

Bozzelli, P. L. (2019). HIV-induced Matrix Metalloproteinases Alter Glial and Neuronal Function (Doctoral dissertation, Georgetown University).
https://repository.library.georgetown.edu/handle/10822/1056018

2018

Whitley, M. J., Henke, D. M., Ghazi, A., Nieman, M., Stoller, M., Simon, L. M., ... & Shaw, C. A. (2018). The protease-activated receptor 4 Ala120Thr variant alters platelet responsiveness to low-dose thrombin and PAR4 desensitization, and is blocked by non-competitive P2Y12 inhibition. Journal of Thrombosis and Haemostasis, 16(12), 2501-2514.
https://onlinelibrary.wiley.com/doi/abs/10.1111/jth.14318

Whitley, M. (2018). The Effect of the PAR4 Ala120Thr Variant on the Platelet Thrombin Response, Receptor Desensitization, and Platelet Antagonists (Doctoral dissertation, Thomas Jefferson University).
http://search.proquest.com/openview/42bf106c797ba82d2fe073dff9d016bf/1?pq-origsite=gscholar&cbl=18750&diss=y

Bielig, I. (2018). Gerinnungsfaktor Xa induziert inflammatorische Prozesse durch die Aktivierung Protease-aktivierter Rezeptoren in humanem Vorhofgewebe.
https://opendata.uni-halle.de/bitstream/1981185920/12339/1/Dissertation_Ines_Bielig.pdf
* GB83 and Vorapaxar from Axon Medchem

White, M. J., Chinea, L. E., Pilling, D., & Gomer, R. H. (2018). Protease activated-receptor 2 is necessary for neutrophil chemorepulsion induced by trypsin, tryptase, or dipeptidyl peptidase IV. Journal of Leukocyte Biology, 103(1), 119-128.
https://onlinelibrary.wiley.com/doi/abs/10.1002/JLB.3A0717-308R

Gupta, N., Sinha, R., Krasnodembskaya, A., Xu, X., Nizet, V., Matthay, M. A., & Griffin, J. H. (2018). The TLR4-PAR1 Axis Regulates Bone Marrow Mesenchymal Stromal Cell Survival and Therapeutic Capacity in Experimental Bacterial Pneumonia. Stem Cells, 36(5), 796-806.
https://stemcellsjournals.onlinelibrary.wiley.com/doi/abs/10.1002/stem.2796

French, S. L., Thalmann, C., Bray, P. F., Macdonald, L. E., Murphy, A. J., Sleeman, M. W., & Hamilton, J. R. (2018). A function-blocking PAR4 antibody is markedly antithrombotic in the face of a hyperreactive PAR4 variant. Blood Advances, 2(11), 1283-1293.
http://www.bloodadvances.org/content/2/11/1283.abstract

Gandhi, D. M., Majewski, M. W., Rosas Jr, R., Kentala, K., Foster, T. J., Greve, E., & Dockendorff, C. (2018). Characterization of Protease-Activated Receptor (PAR) ligands: Parmodulins are reversible allosteric inhibitors of PAR1-driven calcium mobilization in endothelial cells. Bioorganic & Medicinal Chemistry, 26(9), 2514-2529.
https://www.sciencedirect.com/science/article/pii/S0968089618300117
* Vorapaxar, Q94 and E5555 from Axon Medchem

Bray, P., Holinstat, M., & Edelstein, L. (2018). PAR4 inhibitor therapy for patients with PAR4 polymorphism. U.S. Patent Application No. 15/703,739.
https://patents.google.com/patent/US20180000784A1/en

Antoniak, S., Tatsumi, K., Schmedes, C. M., Grover, S. P., Pawlinski, R., & Mackman, N. (2018). Protease-activated receptor 1 activation enhances doxorubicin-induced cardiotoxicity. Journal of Molecular and Cellular Cardiology.
https://www.sciencedirect.com/science/article/pii/S0022282818307818

2017

Gupta, N., Sinha, R., Krasnodembskaya, A., Xu, X., Nizet, V., Matthay, M. A., & Griffin, G. (2017). The TLR4–PAR1 Axis Regulates Bone Marrow Mesenchymal Stromal Cell Survival and Therapeutic Capacity in Murine E. coli Pneumonia.
https://pure.qub.ac.uk/portal/files/139936838/BoneMarrow.pdf

Byskov, K., Boettger, T., Ruehle, P. F., Nielsen, N. V., Etscheid, M., & Kanse, S. M. (2017). Factor VII activating protease (FSAP) regulates the expression of inflammatory genes in vascular smooth muscle and endothelial cells. Atherosclerosis, 265, 133-139.
https://www.sciencedirect.com/science/article/pii/S0021915017312510
* Vorapax and SCH79797 from Axon Medchem

Moschonas, I. C., Kellici, T. F., Mavromoustakos, T., Stathopoulos, P., Tsikaris, V., Magafa, V., ... & Tselepis, A. D. (2017). Molecular requirements involving the human platelet protease-activated receptor-4 mechanism of activation by peptide analogues of its tethered-ligand. Platelets, 28(8), 812-821.
https://www.tandfonline.com/doi/abs/10.1080/09537104.2017.1282607

Bray, P., Holinstat, M., & Edelstein, L. (2017). PAR4 inhibitor therapy for patients with PAR4 polymorphism. U.S. Patent No 9,789,087.
https://patents.google.com/patent/US9789087B2/en

Goldman, S. A., & Auvergne, R. (2017). Use of inhibitors of binding between a PAR-1 receptor and its ligands for the treatment of glioma. U.S. Patent Application No 15/425,562.
https://patents.google.com/patent/US20170281710A1/en

Vinholt, P. J., Frederiksen, H., Hvas, A. M., Sprogoe, U., & Nielsen, C. (2017). Measurement of platelet aggregation, independently of patient platelet count: a flow-cytometric approach. Journal of Thrombosis and Haemostasis.
http://onlinelibrary.wiley.com/doi/10.1111/jth.13675/full

2016

Auvergne, R., Wu, C., Connell, A., Au, S., Cornwell, A., Osipovitch, M., ... & Goldman, S. A. (2016). PAR1 inhibition suppresses the self-renewal and growth of A2B5-defined glioma progenitor cells and their derived gliomas in vivo. Oncogene, 35(29), 3817.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4885796/

Stahn, S., Thelen, L., Albrecht, I. M., Bitzer, J., Henkel, T., & Teusch, N. E. (2016). Teleocidin A2 inhibits human proteinase-activated receptor 2 signaling in tumor cells. Pharmacology Research & Perspectives, 4(4). DOI: 10.1002/prp2.230.
http://onlinelibrary.wiley.com/doi/10.1002/prp2.230/full

Bray, P., Holinstat, M., & Edelstein, L. (2016). PAR4 inhibitor therapy for patients with PAR4 polymorphism. U.S. Patent Application No. 15/226,425.
https://www.google.com/patents/US20170035734

Palekar, R. U., Vemuri, C., Marsh, J. N., Arif, B., & Wickline, S. A. (2016). Antithrombin nanoparticles inhibit stent thrombosis in ex vivo static and flow models. Journal of Vascular Surgery, 64(5), 1459-1467.
http://www.sciencedirect.com/science/article/pii/S0741521415018364

2013 to 2015

Kim, H. N., Kim, Y. R., Ahn, S. M., Lee, S. K., Shin, H. K., & Choi, B. T. (2015). Protease-activated receptor-1 antagonist ameliorates the clinical symptoms of experimental autoimmune encephalomyelitis via inhibiting breakdown of blood–brain barrier. Journal of Neurochemistry, 135(3), 577-588.
http://onlinelibrary.wiley.com/doi/10.1111/jnc.13285/full

Goldman, S. A., & Auvergne, R. (2014). Use of inhibitors of binding between a PAR-1 receptor and its ligands for the treatment of glioma. U.S. Patent Application No. 14/776,961.
https://www.google.com/patents/US20160045506

José, R. J., Williams, A. E., Mercer, P. F., Sulikowski, M. G., Brown, J. S., & Chambers, R. C. (2015). Regulation of neutrophilic inflammation by proteinase-activated receptor 1 during bacterial pulmonary infection. The Journal of Immunology, 194(12), 6024-6034.
http://www.jimmunol.org/content/194/12/6024.short
http://www.jimmunol.org/content/jimmunol/194/12/6024.full.pdf

White, M. J., Galvis-Carvajal, E., & Gomer, R. H. (2015). A brief exposure to tryptase or thrombin potentiates fibrocyte differentiation in the presence of serum or serum amyloid p. The Journal of Immunology, 194(1), 142-150.
http://www.jimmunol.org/content/194/1/142.short
(* SCH79797 and Vorapaxar from Axon Medchem)

Aisiku, O., Peters, C. G., De Ceunynck, K., Ghosh, C. C., Dilks, J. R., Fustolo-Gunnink, S. F., ... & Flaumenhaft, R. (2015). Parmodulins inhibit thrombus formation without inducing endothelial injury caused by vorapaxar. Blood, 125(12), 1976-1985.
http://www.bloodjournal.org/content/125/12/1976?sso-checked=true

Edelstein, L. C., Simon, L. M., Lindsay, C. R., Kong, X., Teruel-Montoya, R., Tourdot, B. E., ... & Holinstat, M. (2014). Common variants in the human platelet PAR4 thrombin receptor alter platelet function and differ by race. Blood, 124(23), 3450-3458.
http://www.bloodjournal.org/content/124/23/3450

Zhao, F., Guo, X., Wang, Y., Liu, J., Lee, W. H., & Zhang, Y. (2014). Drug target mining and analysis of the Chinese tree shrew for pharmacological testing. PLoS One, 9(8), e104191.
http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0104191

Smoktunowicz, N. (2014). Procoagulant signalling in lung injury and fibrosis (Doctoral dissertation, UCL (University College London)).
http://discovery.ucl.ac.uk/1435049/1/NS%20Procoagulant%20signalling%20in%20lung%20injury%20and%20fibrosis%20FINAL%20SUBMISSON%20July%202014.pdf
(* GB83 and Vorapaxar from Axon Medchem)

Huang, S. C. (2014). Proteinase-activated receptor-1 (PAR1) and PAR2 mediate relaxation of guinea pig internal anal sphincter. Regulatory Peptides, 189, 46-50.
http://www.sciencedirect.com/science/article/pii/S0167011514000226
(* GB83 and Vorapaxar from Axon Medchem)

Aerts, L., Hamelin, M. È., Rhéaume, C., Lavigne, S., Couture, C., Kim, W., ... & Riteau, B. (2013). Modulation of protease activated receptor 1 influences human metapneumovirus disease severity in a mouse model. PLoS One, 8(8), e72529.
http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0072529
(* SCH79797 and Vorapaxar from Axon Medchem)