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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.


MALT1 is a critical mediator of PAR1-driven NF-κB activation and metastasis in multiple tumor types.

McAuley JR, Bailey KM, Ekambaram P, Klei LR, Kang H, Hu D, Freeman TJ, Concel VJ, Hubel NE, Lee JL, Klei HB, Cheng J, Sekar P, Bridwell RE, Covic L, Lucas PC, McAllister-Lucas LM.

Oncogene. 2019 Dec;38(49):7384-7398. doi: 10.1038/s41388-019-0958-4. Epub 2019 Aug 16.


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.


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.


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.


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.


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.


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.


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.


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.


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.


Proteinase-activated receptor-1-triggered activation of tumor progression locus-2 promotes actin cytoskeleton reorganization and cell migration.

Hatziapostolou M, Polytarchou C, Panutsopulos D, Covic L, Tsichlis PN.

Cancer Res. 2008 Mar 15;68(6):1851-61. doi: 10.1158/0008-5472.CAN-07-5793.


'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.


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.


PAR1 is a matrix metalloprotease-1 receptor that promotes invasion and tumorigenesis of breast cancer cells.

Boire A, Covic L, Agarwal A, Jacques S, Sherifi S, Kuliopulos A.

Cell. 2005 Feb 11;120(3):303-13.


Effect of selective inhibition of the p38 MAP kinase pathway on platelet aggregation.

Kuliopulos A, Mohanlal R, Covic L.

Thromb Haemost. 2004 Dec;92(6):1387-93.


Structural basis for thrombin activation of a protease-activated receptor: inhibition of intramolecular liganding.

Seeley S, Covic L, Jacques SL, Sudmeier J, Baleja JD, Kuliopulos A.

Chem Biol. 2003 Nov;10(11):1033-41.


Blocking receptors on the inside: pepducin-based intervention of PAR signaling and thrombosis.

Kuliopulos A, Covic L.

Life Sci. 2003 Dec 5;74(2-3):255-62. Erratum in: Life Sci. 2012 Sep 4;91(5-6):221.


Pepducin-based intervention of thrombin-receptor signaling and systemic platelet activation.

Covic L, Misra M, Badar J, Singh C, Kuliopulos A.

Nat Med. 2002 Oct;8(10):1161-5. Epub 2002 Sep 23.


Activation and inhibition of G protein-coupled receptors by cell-penetrating membrane-tethered peptides.

Covic L, Gresser AL, Talavera J, Swift S, Kuliopulos A.

Proc Natl Acad Sci U S A. 2002 Jan 22;99(2):643-8.


Biphasic kinetics of activation and signaling for PAR1 and PAR4 thrombin receptors in platelets.

Covic L, Gresser AL, Kuliopulos A.

Biochemistry. 2000 May 9;39(18):5458-67.


PAR1 thrombin receptor-G protein interactions. Separation of binding and coupling determinants in the galpha subunit.

Swift S, Sheridan PJ, Covic L, Kuliopulos A.

J Biol Chem. 2000 Jan 28;275(4):2627-35.


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