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PAR2 controls cholesterol homeostasis and lipid metabolism in nonalcoholic fatty liver disease.

Rana R, Shearer AM, Fletcher EK, Nguyen N, Guha S, Cox DH, Abdelmalek M, Wang Y, Baleja JD, Covic L, Kuliopulos A.

Mol Metab. 2019 Nov;29:99-113. doi: 10.1016/j.molmet.2019.08.019. Epub 2019 Aug 28.


Effects of vorapaxar on clot characteristics, coagulation, inflammation, and platelet and endothelial function in patients treated with mono- and dual-antiplatelet therapy.

Bliden K, Chaudhary R, Kuliopulos A, Tran H, Taheri H, Tehrani B, Rosenblatt A, Navarese E, Tantry US, Gurbel PA.

J Thromb Haemost. 2020 Jan;18(1):23-35. doi: 10.1111/jth.14616. Epub 2019 Sep 17.


Enhanced potency of prasugrel on protease-activated receptors following bivalirudin treatment for PCI as compared to clopidogrel.

Kimmelstiel C, Stevenson R, Nguyen N, Van Doren L, Zhang P, Perkins J, Kapur NK, Weintraub A, Castaneda V, Kuliopulos A, Covic L.

Thromb Res. 2019 May;177:59-69. doi: 10.1016/j.thromres.2019.01.017. Epub 2019 Feb 13.


Atorvastatin Decreases Renal Menaquinone-4 Formation in C57BL/6 Male Mice.

Harshman SG, Shea MK, Fu X, Grusak MA, Smith D, Lamon-Fava S, Kuliopulos A, Greenberg A, Booth SL.

J Nutr. 2019 Mar 1;149(3):416-421. doi: 10.1093/jn/nxy290.


Trace amine-associated receptor 1 (TAAR1) promotes anti-diabetic signaling in insulin-secreting cells.

Michael ES, Covic L, Kuliopulos A.

J Biol Chem. 2019 Mar 22;294(12):4401-4411. doi: 10.1074/jbc.RA118.005464. Epub 2019 Jan 22.


PAR2 Pepducin-Based Suppression of Inflammation and Itch in Atopic Dermatitis Models.

Barr TP, Garzia C, Guha S, Fletcher EK, Nguyen N, Wieschhaus AJ, Ferrer L, Covic L, Kuliopulos A.

J Invest Dermatol. 2019 Feb;139(2):412-421. doi: 10.1016/j.jid.2018.08.019. Epub 2018 Oct 1.


Protease-Activated Receptor 1 as Therapeutic Target in Breast, Lung, and Ovarian Cancer: Pepducin Approach.

Covic L, Kuliopulos A.

Int J Mol Sci. 2018 Jul 31;19(8). pii: E2237. doi: 10.3390/ijms19082237. Review.


Noncanonical Matrix Metalloprotease 1-Protease-Activated Receptor 1 Signaling Drives Progression of Atherosclerosis.

Rana R, Huang T, Koukos G, Fletcher EK, Turner SE, Shearer A, Gurbel PA, Rade JJ, Kimmelstiel CD, Bliden KP, Covic L, Kuliopulos A.

Arterioscler Thromb Vasc Biol. 2018 Jun;38(6):1368-1380. doi: 10.1161/ATVBAHA.118.310967. Epub 2018 Apr 5.


Atherothrombosis and Thromboembolism: Position Paper from the Second Maastricht Consensus Conference on Thrombosis.

Spronk HMH, Padro T, Siland JE, Prochaska JH, Winters J, van der Wal AC, Posthuma JJ, Lowe G, d'Alessandro E, Wenzel P, Coenen DM, Reitsma PH, Ruf W, van Gorp RH, Koenen RR, Vajen T, Alshaikh NA, Wolberg AS, Macrae FL, Asquith N, Heemskerk J, Heinzmann A, Moorlag M, Mackman N, van der Meijden P, Meijers JCM, Heestermans M, Renné T, Dólleman S, Chayouâ W, Ariëns RAS, Baaten CC, Nagy M, Kuliopulos A, Posma JJ, Harrison P, Vries MJ, Crijns HJGM, Dudink EAMP, Buller HR, Henskens YMC, Själander A, Zwaveling S, Erküner O, Eikelboom JW, Gulpen A, Peeters FECM, Douxfils J, Olie RH, Baglin T, Leader A, Schotten U, Scaf B, van Beusekom HMM, Mosnier LO, van der Vorm L, Declerck P, Visser M, Dippel DWJ, Strijbis VJ, Pertiwi K, Ten Cate-Hoek AJ, Ten Cate H.

Thromb Haemost. 2018 Feb;118(2):229-250. doi: 10.1160/TH17-07-0492. Epub 2018 Jan 29.


Targeting Liver Fibrosis with a Cell-penetrating Protease-activated Receptor-2 (PAR2) Pepducin.

Shearer AM, Rana R, Austin K, Baleja JD, Nguyen N, Bohm A, Covic L, Kuliopulos A.

J Biol Chem. 2016 Oct 28;291(44):23188-23198. Epub 2016 Sep 9.


Tissue Concentrations of Vitamin K and Expression of Key Enzymes of Vitamin K Metabolism Are Influenced by Sex and Diet but Not Housing in C57Bl6 Mice.

Harshman SG, Fu X, Karl JP, Barger K, Lamon-Fava S, Kuliopulos A, Greenberg AS, Smith D, Shen X, Booth SL.

J Nutr. 2016 Aug;146(8):1521-7. doi: 10.3945/jn.116.233130. Epub 2016 Jul 6.


Reversal of murine alcoholic steatohepatitis by pepducin-based functional blockade of interleukin-8 receptors.

Wieser V, Adolph TE, Enrich B, Kuliopulos A, Kaser A, Tilg H, Kaneider NC.

Gut. 2017 May;66(5):930-938. doi: 10.1136/gutjnl-2015-310344. Epub 2016 Feb 8.


Cell-Penetrating Pepducin Therapy Targeting PAR1 in Subjects With Coronary Artery Disease.

Gurbel PA, Bliden KP, Turner SE, Tantry US, Gesheff MG, Barr TP, Covic L, Kuliopulos A.

Arterioscler Thromb Vasc Biol. 2016 Jan;36(1):189-97. doi: 10.1161/ATVBAHA.115.306777.


Pepducins and Other Lipidated Peptides as Mechanistic Probes and Therapeutics.

Zhang P, Covic L, Kuliopulos A.

Methods Mol Biol. 2015;1324:191-203. doi: 10.1007/978-1-4939-2806-4_13.


Dysregulated protease activated receptor 1 (PAR1) promotes metastatic phenotype in breast cancer through HMGA2.

Yang E, Cisowski J, Nguyen N, O'Callaghan K, Xu J, Agarwal A, Kuliopulos A, Covic L.

Oncogene. 2016 Mar 24;35(12):1529-40. doi: 10.1038/onc.2015.217. Epub 2015 Jul 13.


Allosteric Activation of a G Protein-coupled Receptor with Cell-penetrating Receptor Mimetics.

Zhang P, Leger AJ, Baleja JD, Rana R, Corlin T, Nguyen N, Koukos G, Bohm A, Covic L, Kuliopulos A.

J Biol Chem. 2015 Jun 19;290(25):15785-98. doi: 10.1074/jbc.M115.636316. Epub 2015 May 1.


G-protein-coupled receptors signaling pathways in new antiplatelet drug development.

Gurbel PA, Kuliopulos A, Tantry US.

Arterioscler Thromb Vasc Biol. 2015 Mar;35(3):500-12. doi: 10.1161/ATVBAHA.114.303412. Epub 2015 Jan 29. Review.


Mouse matrix metalloprotease-1a (Mmp1a) gives new insight into MMP function.

Foley CJ, Kuliopulos A.

J Cell Physiol. 2014 Dec;229(12):1875-80. doi: 10.1002/jcp.24650. Review.


Noncanonical matrix metalloprotease-1-protease-activated receptor-1 signaling triggers vascular smooth muscle cell dedifferentiation and arterial stenosis.

Austin KM, Nguyen N, Javid G, Covic L, Kuliopulos A.

J Biol Chem. 2013 Aug 9;288(32):23105-15. doi: 10.1074/jbc.M113.467019. Epub 2013 Jun 27.


Matrix metalloprotease 1a deficiency suppresses tumor growth and angiogenesis.

Foley CJ, Fanjul-Fernández M, Bohm A, Nguyen N, Agarwal A, Austin K, Koukos G, Covic L, López-Otín C, Kuliopulos A.

Oncogene. 2014 Apr 24;33(17):2264-72. doi: 10.1038/onc.2013.157. Epub 2013 May 27.


Selective blockade of matrix metalloprotease-14 with a monoclonal antibody abrogates invasion, angiogenesis, and tumor growth in ovarian cancer.

Kaimal R, Aljumaily R, Tressel SL, Pradhan RV, Covic L, Kuliopulos A, Zarwan C, Kim YB, Sharifi S, Agarwal A.

Cancer Res. 2013 Apr 15;73(8):2457-2467. doi: 10.1158/0008-5472.CAN-12-1426. Epub 2013 Feb 19.


Pharmacological inhibition of PAR2 with the pepducin P2pal-18S protects mice against acute experimental biliary pancreatitis.

Michael ES, Kuliopulos A, Covic L, Steer ML, Perides G.

Am J Physiol Gastrointest Liver Physiol. 2013 Mar 1;304(5):G516-26. doi: 10.1152/ajpgi.00296.2012. Epub 2012 Dec 28.


Matrix metalloproteases and PAR1 activation.

Austin KM, Covic L, Kuliopulos A.

Blood. 2013 Jan 17;121(3):431-9. doi: 10.1182/blood-2012-09-355958. Epub 2012 Oct 18. Review.


Suppression of arterial thrombosis without affecting hemostatic parameters with a cell-penetrating PAR1 pepducin.

Zhang P, Gruber A, Kasuda S, Kimmelstiel C, O'Callaghan K, Cox DH, Bohm A, Baleja JD, Covic L, Kuliopulos A.

Circulation. 2012 Jul 3;126(1):83-91. doi: 10.1161/CIRCULATIONAHA.112.091918. Epub 2012 Jun 15.


Matrix metalloprotease-1a promotes tumorigenesis and metastasis.

Foley CJ, Luo C, O'Callaghan K, Hinds PW, Covic L, Kuliopulos A.

J Biol Chem. 2012 Jul 13;287(29):24330-8. doi: 10.1074/jbc.M112.356303. Epub 2012 May 9.


Turning receptors on and off with intracellular pepducins: new insights into G-protein-coupled receptor drug development.

O'Callaghan K, Kuliopulos A, Covic L.

J Biol Chem. 2012 Apr 13;287(16):12787-96. doi: 10.1074/jbc.R112.355461. Epub 2012 Feb 28. Review.


Targeting CXCR4 with cell-penetrating pepducins in lymphoma and lymphocytic leukemia.

O'Callaghan K, Lee L, Nguyen N, Hsieh MY, Kaneider NC, Klein AK, Sprague K, Van Etten RA, Kuliopulos A, Covic L.

Blood. 2012 Feb 16;119(7):1717-25. doi: 10.1182/blood-2011-04-347518. Epub 2011 Dec 20.


Protease-activated receptor-2 modulates protease-activated receptor-1-driven neointimal hyperplasia.

Sevigny LM, Austin KM, Zhang P, Kasuda S, Koukos G, Sharifi S, Covic L, Kuliopulos A.

Arterioscler Thromb Vasc Biol. 2011 Dec;31(12):e100-6. doi: 10.1161/ATVBAHA.111.238261. Epub 2011 Sep 22.


Tumor progression locus 2 mediates signal-induced increases in cytoplasmic calcium and cell migration.

Hatziapostolou M, Koukos G, Polytarchou C, Kottakis F, Serebrennikova O, Kuliopulos A, Tsichlis PN.

Sci Signal. 2011 Aug 23;4(187):ra55. doi: 10.1126/scisignal.2002006.


Targeting protease-activated receptor-1 with cell-penetrating pepducins in lung cancer.

Cisowski J, O'Callaghan K, Kuliopulos A, Yang J, Nguyen N, Deng Q, Yang E, Fogel M, Tressel S, Foley C, Agarwal A, Hunt SW 3rd, McMurry T, Brinckerhoff L, Covic L.

Am J Pathol. 2011 Jul;179(1):513-23. doi: 10.1016/j.ajpath.2011.03.025. Epub 2011 May 7.


G protein-coupled receptor modulation with pepducins: moving closer to the clinic.

Dimond P, Carlson K, Bouvier M, Gerard C, Xu L, Covic L, Agarwal A, Ernst OP, Janz JM, Schwartz TW, Gardella TJ, Milligan G, Kuliopulos A, Sakmar TP, Hunt SW 3rd.

Ann N Y Acad Sci. 2011 May;1226:34-49. doi: 10.1111/j.1749-6632.2011.06039.x.


A matrix metalloprotease-PAR1 system regulates vascular integrity, systemic inflammation and death in sepsis.

Tressel SL, Kaneider NC, Kasuda S, Foley C, Koukos G, Austin K, Agarwal A, Covic L, Opal SM, Kuliopulos A.

EMBO Mol Med. 2011 Jul;3(7):370-84. doi: 10.1002/emmm.201100145. Epub 2011 May 18.


Serine and metalloprotease signaling through PAR1 in arterial thrombosis and vascular injury.

Koukos G, Sevigny L, Zhang P, Covic L, Kuliopulos A.

IUBMB Life. 2011 Jun;63(6):412-8. doi: 10.1002/iub.465. Epub 2011 May 9. Review.


Interdicting protease-activated receptor-2-driven inflammation with cell-penetrating pepducins.

Sevigny LM, Zhang P, Bohm A, Lazarides K, Perides G, Covic L, Kuliopulos A.

Proc Natl Acad Sci U S A. 2011 May 17;108(20):8491-6. doi: 10.1073/pnas.1017091108. Epub 2011 May 2.


Bivalirudin is a dual inhibitor of thrombin and collagen-dependent platelet activation in patients undergoing percutaneous coronary intervention.

Kimmelstiel C, Zhang P, Kapur NK, Weintraub A, Krishnamurthy B, Castaneda V, Covic L, Kuliopulos A.

Circ Cardiovasc Interv. 2011 Apr 1;4(2):171-9. doi: 10.1161/CIRCINTERVENTIONS.110.959098. Epub 2011 Mar 1.


Identification of an antithrombotic allosteric modulator that acts through helix 8 of PAR1.

Dowal L, Sim DS, Dilks JR, Blair P, Beaudry S, Denker BM, Koukos G, Kuliopulos A, Flaumenhaft R.

Proc Natl Acad Sci U S A. 2011 Feb 15;108(7):2951-6. doi: 10.1073/pnas.1014863108. Epub 2011 Jan 31.


Pharmacology, biodistribution, and efficacy of GPCR-based pepducins in disease models.

Tressel SL, Koukos G, Tchernychev B, Jacques SL, Covic L, Kuliopulos A.

Methods Mol Biol. 2011;683:259-75. doi: 10.1007/978-1-60761-919-2_19. Review.


Identification of a metalloprotease-chemokine signaling system in the ovarian cancer microenvironment: implications for antiangiogenic therapy.

Agarwal A, Tressel SL, Kaimal R, Balla M, Lam FH, Covic L, Kuliopulos A.

Cancer Res. 2010 Jul 15;70(14):5880-90. doi: 10.1158/0008-5472.CAN-09-4341. Epub 2010 Jun 22.


A novel protease-activated receptor-1 interactor, Bicaudal D1, regulates G protein signaling and internalization.

Swift S, Xu J, Trivedi V, Austin KM, Tressel SL, Zhang L, Covic L, Kuliopulos A.

J Biol Chem. 2010 Apr 9;285(15):11402-10. doi: 10.1074/jbc.M110.105403. Epub 2010 Feb 17.


Insider access: pepducin symposium explores a new approach to GPCR modulation.

Miller J, Agarwal A, Devi LA, Fontanini K, Hamilton JA, Pin JP, Shields DC, Spek CA, Sakmar TP, Kuliopulos A, Hunt SW 3rd.

Ann N Y Acad Sci. 2009 Nov;1180 Suppl 1:E1-12. doi: 10.1111/j.1749-6632.2009.05326.x.


Blockade of PAR1 signaling with cell-penetrating pepducins inhibits Akt survival pathways in breast cancer cells and suppresses tumor survival and metastasis.

Yang E, Boire A, Agarwal A, Nguyen N, O'Callaghan K, Tu P, Kuliopulos A, Covic L.

Cancer Res. 2009 Aug 1;69(15):6223-31. doi: 10.1158/0008-5472.CAN-09-0187. Epub 2009 Jul 21.


Platelet matrix metalloprotease-1 mediates thrombogenesis by activating PAR1 at a cryptic ligand site.

Trivedi V, Boire A, Tchernychev B, Kaneider NC, Leger AJ, O'Callaghan K, Covic L, Kuliopulos A.

Cell. 2009 Apr 17;137(2):332-43. doi: 10.1016/j.cell.2009.02.018.


G-protein-coupled receptors as signaling targets for antiplatelet therapy.

Smyth SS, Woulfe DS, Weitz JI, Gachet C, Conley PB, Goodman SG, Roe MT, Kuliopulos A, Moliterno DJ, French PA, Steinhubl SR, Becker RC; 2008 Platelet Colloquium Participants.

Arterioscler Thromb Vasc Biol. 2009 Apr;29(4):449-57. doi: 10.1161/ATVBAHA.108.176388. Epub 2008 Nov 20. Review.


Targeting a metalloprotease-PAR1 signaling system with cell-penetrating pepducins inhibits angiogenesis, ascites, and progression of ovarian cancer.

Agarwal A, Covic L, Sevigny LM, Kaneider NC, Lazarides K, Azabdaftari G, Sharifi S, Kuliopulos A.

Mol Cancer Ther. 2008 Sep;7(9):2746-57. doi: 10.1158/1535-7163.MCT-08-0177.


'Role reversal' for the receptor PAR1 in sepsis-induced vascular damage.

Kaneider NC, Leger AJ, Agarwal A, Nguyen N, Perides G, Derian C, Covic L, Kuliopulos A.

Nat Immunol. 2007 Dec;8(12):1303-12. Epub 2007 Oct 28.


Therapeutic targeting of molecules involved in leukocyte-endothelial cell interactions.

Kaneider NC, Leger AJ, Kuliopulos A.

FEBS J. 2006 Oct;273(19):4416-24. Epub 2006 Sep 5. Review.


Protease-activated receptors in cardiovascular diseases.

Leger AJ, Covic L, Kuliopulos A.

Circulation. 2006 Sep 5;114(10):1070-7. Review.


Blocking the protease-activated receptor 1-4 heterodimer in platelet-mediated thrombosis.

Leger AJ, Jacques SL, Badar J, Kaneider NC, Derian CK, Andrade-Gordon P, Covic L, Kuliopulos A.

Circulation. 2006 Mar 7;113(9):1244-54. Epub 2006 Feb 27.


Role of the PAR1 receptor 8th helix in signaling: the 7-8-1 receptor activation mechanism.

Swift S, Leger AJ, Talavera J, Zhang L, Bohm A, Kuliopulos A.

J Biol Chem. 2006 Feb 17;281(7):4109-16. Epub 2005 Dec 13.

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