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Items: 1 to 20 of 79

1.

Design, synthesis and biological evaluation of new peptide-based ureas and thioureas as potential antagonists of the thrombin receptor PAR1.

Ventosa-Andrés P, Valdivielso AM, Pappos I, García-López MT, Tsopanoglou NE, Herranz R.

Eur J Med Chem. 2012 Dec;58:98-111. doi: 10.1016/j.ejmech.2012.10.015. Epub 2012 Oct 17.

PMID:
23123726
2.
3.

Highly functionalized 2-oxopiperazine-based peptidomimetics: an approach to PAR1 antagonists.

Valdivielso ÁM, Ventosa-Andrés P, Tato F, Fernández-Ibañez MÁ, Pappos I, Tsopanoglou NE, García-López MT, Gutiérrez-Rodríguez M, Herranz R.

Eur J Med Chem. 2013;70:199-224. doi: 10.1016/j.ejmech.2013.09.058. Epub 2013 Oct 10.

PMID:
24158013
4.

Exploring the Phe-Gly dipeptide-derived piperazinone scaffold in the search for antagonists of the thrombin receptor PAR1.

Valdivielso ÁM, García-López MT, Gutiérrez-Rodríguez M, Herranz R.

Molecules. 2014 Apr 16;19(4):4814-46. doi: 10.3390/molecules19044814.

5.

Protease-activated receptor-2 (PAR-2): structure-function study of receptor activation by diverse peptides related to tethered-ligand epitopes.

Maryanoff BE, Santulli RJ, McComsey DF, Hoekstra WJ, Hoey K, Smith CE, Addo M, Darrow AL, Andrade-Gordon P.

Arch Biochem Biophys. 2001 Feb 15;386(2):195-204.

PMID:
11368342
6.

The preparation and characterization of novel peptide antagonists to thrombin and factor VIIa and activation of protease-activated receptor 1.

Nieman MT, Warnock M, Hasan AA, Mahdi F, Lucchesi BR, Brown NJ, Murphey LJ, Schmaier AH.

J Pharmacol Exp Ther. 2004 Nov;311(2):492-501. Epub 2004 Jun 21.

PMID:
15210836
7.

Synthesis and biological evaluation of piperazinyl carbamates and ureas as fatty acid amide hydrolase (FAAH) and transient receptor potential (TRP) channel dual ligands.

Morera E, De Petrocellis L, Morera L, Moriello AS, Ligresti A, Nalli M, Woodward DF, Di Marzo V, Ortar G.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6806-9. doi: 10.1016/j.bmcl.2009.09.033. Epub 2009 Oct 20.

PMID:
19875281
8.

Non-peptidic small-molecule antagonists of the human platelet thrombin receptor PAR-1.

Selnick HG, Barrow JC, Nantermet PG, Connolly TM.

Curr Med Chem Cardiovasc Hematol Agents. 2003 Mar;1(1):47-59. Review.

PMID:
15317290
9.

Design, synthesis and biological evaluation of non-peptide PAR1 thrombin receptor antagonists based on small bifunctional templates: arginine and phenylalanine side chain groups are keys for receptor activity.

Androutsou ME, Saifeddine M, Hollenberg MD, Matsoukas J, Agelis G.

Amino Acids. 2010 Apr;38(4):985-90. doi: 10.1007/s00726-009-0306-z. Epub 2009 May 31.

PMID:
19484400
10.

Effect of aprotinin and recombinant variants on platelet protease-activated receptor 1 activation.

Day JR, Haskard DO, Taylor KM, Landis RC.

Ann Thorac Surg. 2006 Feb;81(2):619-24.

PMID:
16427862
11.

Chemically modified thrombin and anhydrothrombin that differentiate macromolecular substrates of thrombin.

Hosokawa K, Ohnishi T, Kawakami A, Wakabayashi S, Koide T.

J Thromb Haemost. 2005 Dec;3(12):2703-11. Epub 2005 Oct 25.

12.

Identification of an active metabolite of PAR-1 antagonist RWJ-58259 and synthesis of analogues to enhance its metabolic stability.

Robinson E, Knight E, Smoktunowicz N, Chambers RC, Inglis GG, Chudasama V, Caddick S.

Org Biomol Chem. 2016 Mar 28;14(12):3198-201. doi: 10.1039/c6ob00332j.

PMID:
26927018
13.

Discovery of potent peptide-mimetic antagonists for the human thrombin receptor, protease-activated receptor-1 (PAR-1).

Maryanoff BE, Zhang HC, Andrade-Gordon P, Derian CK.

Curr Med Chem Cardiovasc Hematol Agents. 2003 Mar;1(1):13-36. Review.

PMID:
15317288
14.

Blockade of the thrombin receptor protease-activated receptor-1 with a small-molecule antagonist prevents thrombus formation and vascular occlusion in nonhuman primates.

Derian CK, Damiano BP, Addo MF, Darrow AL, D'Andrea MR, Nedelman M, Zhang HC, Maryanoff BE, Andrade-Gordon P.

J Pharmacol Exp Ther. 2003 Feb;304(2):855-61. Erratum in: J Pharmacol Exp Ther. 2003 Apr;305(1):402.

PMID:
12538843
15.

Synthesis and pharmacological evaluation of peptide-mimetic protease-activated receptor-1 antagonists containing novel heterocyclic scaffolds.

Severino B, Fiorino F, Perissutti E, Frecentese F, Cirino G, Roviezzo F, Santagada V, Caliendo G.

Bioorg Med Chem. 2008 Jun 1;16(11):6009-20. doi: 10.1016/j.bmc.2008.04.059. Epub 2008 Apr 26.

PMID:
18477511
16.

RWJ-58259: a selective antagonist of protease activated receptor-1.

Damiano BP, Derian CK, Maryanoff BE, Zhang HC, Gordon PA.

Cardiovasc Drug Rev. 2003 Winter;21(4):313-26. Review.

PMID:
14647534
17.

Proteinase-activated receptors (PARs)--the PAR3 Neo-N-terminal peptide TFRGAP interacts with PAR1.

Kaufmann R, Schulze B, Krause G, Mayr LM, Settmacher U, Henklein P.

Regul Pept. 2005 Feb 15;125(1-3):61-6.

PMID:
15582715
18.
19.

Inhibition of PAR4 signaling mediates ethanol-induced attenuation of platelet function in vitro.

Kasuda S, Sakurai Y, Shima M, Morimura Y, Kudo R, Takeda T, Ishitani A, Yoshioka A, Hatake K.

Alcohol Clin Exp Res. 2006 Sep;30(9):1608-14.

PMID:
16930224
20.

Characterization of Protease-Activated Receptor (PAR) ligands: Parmodulins are reversible allosteric inhibitors of PAR1-driven calcium mobilization in endothelial cells.

Gandhi DM, Majewski MW, Rosas R Jr, Kentala K, Foster TJ, Greve E, Dockendorff C.

Bioorg Med Chem. 2018 May 15;26(9):2514-2529. doi: 10.1016/j.bmc.2018.04.016. Epub 2018 Apr 6.

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