Results 271 to 280 of about 410,064 (307)

Aptamer Inhibits Degradation of Platelet Proteolytically Activatable Receptor, PAR-1, by Thrombin

Thrombosis Research, 2001
We investigated the in vitro effects of the site-directed thrombin inhibitor-a single-stranded oligonucleotide aptamer (GGTTGGTGTGGTTGG)-on thrombin proteolytic activity towards its two natural substrates: fibrinogen and platelet thrombin receptor (PAR-1).
M A, Boncler, M, Koziolkiewicz, C, Watala   +2 more
openaire   +2 more sources

Effect of Statins on Platelet PAR-1 Thrombin Receptor in Patients With the Metabolic Syndrome (From the PAR-1 Inhibition by Statins [PARIS] Study)

The American Journal of Cardiology, 2006
We investigated whether, in primary prevention patients with metabolic syndrome, statins affect the platelet protease-activated receptor-1 (PAR-1) thrombin receptor by performing serial measurements of its activity and the antigen expression level by flow cytometry before and during treatment.
Victor L, Serebruany, Michael, Miller, Alex N, Pokov, Alex I, Malinin, David R, Lowry, Jean-Francois, Tanguay, Charles H, Hennekens   +6 more
openaire   +2 more sources

Protease Activated Receptor-1 (PAR-1) Impedes Tumor Progression

Blood, 2016
Abstract Activation of cell signaling by thrombin through Protease Activated Receptor-1 (PAR-1) represents one important interface between blood coagulation and cell activation in response to injury and inflammation. In the context of cancer, PAR-1 has been suggested to promote tumor growth through mechanisms coupled to tumor cell ...
Gregory N. Adams, Haley Weston, Leah Rosenfeldt, Malinda Frederick, Joseph S. Palumbo   +4 more
openaire   +1 more source

Discovery of Potent Peptide-Mimetic Antagonists for the Human Thrombin Receptor, Protease-Activated Receptor-1 (PAR-1)

Current Medicinal Chemistry-Cardiovascular & Hematological Agents, 2003
Protease-activated receptors (PARs) represent a unique family of seven-transmembrane G-protein-coupled receptors, which are enzymatically cleaved to expose a new extracellular N-terminus that acts as a tethered activating ligand. PAR-1 is cleaved and activated by the serine protease alpha-thrombin, is expressed in various tissues (e.g.
Bruce E, Maryanoff, Han-Cheng, Zhang, Patricia, Andrade-Gordon, Claudia K, Derian   +3 more
openaire   +2 more sources

Thrombin receptor (PAR-1) antagonists. Heterocycle-based peptidomimetics of the SFLLR agonist motif

Bioorganic & Medicinal Chemistry Letters, 1998
The thrombin receptor (PAR-1) is activated by alpha-thrombin to stimulate various cell types, including platelets, through the tethered-ligand sequence SFLLRN. A series of azole-based carboxamides, designed after SFLLR, were synthesized and evaluated in vitro.
W J, Hoekstra, B L, Hulshizer, D F, McComsey, P, Andrade-Gordon, J A, Kauffman, M F, Addo, D, Oksenberg, R M, Scarborough, B E, Maryanoff   +8 more
openaire   +2 more sources

Heterocycle-peptide hybrid compounds. Aminotriazole-containing agonists of the thrombin receptor (PAR-1)

Bioorganic & Medicinal Chemistry Letters, 1999
The thrombin receptor PAR-1 is activated by alpha-thrombin to stimulate cells, including platelets, through the tethered-ligand sequence SFLLRN. We have discovered a novel series of heterocycle-peptide hybrids comprised of a tripeptide segment, such as Cha-Arg-Phe, and an N-terminal heterocyclic group, many of which behave as full PAR-1 agonists ...
D F, McComsey, M J, Hawkins, P, Andrade-Gordon, M F, Addo, D, Oksenberg, B E, Maryanoff   +5 more
openaire   +2 more sources

Activation of the small GTPases, rac and cdc42, after ligation of the platelet PAR-1 receptor

Blood, 2000
Stimulation of platelet PAR-1 receptors results in the rapid (10 to 30 seconds) and extensive (30% to 40% of total) guanosine triphosphate (GTP) charging of endogenous platelet rac, previously identified as a possible key intermediate in the signal pathway between PAR-1 and actin filament barbed-end uncapping, leading to actin assembly.
A C, Azim, K, Barkalow, J, Chou, J H, Hartwig   +3 more
openaire   +2 more sources

Vorapaxar, an oral PAR-1 receptor antagonist, does not affect the pharmacokinetics and pharmacodynamics of warfarin

European Journal of Clinical Pharmacology, 2012
Vorapaxar is an orally active protease-activated receptor 1 (PAR-1) antagonist that inhibits thrombin-induced platelet aggregation. This open-label study assessed the pharmacokinetics and pharmacodynamics of single-dose warfarin in the presence/absence of multiple-dose vorapaxar in 12 healthy men.Subjects received two treatments separated by ≥ 7-day ...
Teddy, Kosoglou, Yali, Zhu, Fengjuan, Xuan, Laura, Black, Amy O, Johnson-Levonas, Monika, Martinho, Paul, Statkevich, David L, Cutler   +7 more
openaire   +2 more sources

Discovery and synthesis of a novel series of quinoline-based thrombin receptor (PAR-1) antagonists

Bioorganic & Medicinal Chemistry Letters, 2006
The design, synthesis, and SAR studies of a structurally novel series of highly potent thrombin receptor (PAR-1) antagonists are described. Compound 30 is a highly potent thrombin receptor antagonist (IC(50)=6.3 nM), a related compound 36 showing efficacy in a monkey ex vivo study.
Martin C, Clasby, Samuel, Chackalamannil, Michael, Czarniecki, Dario, Doller, Keith, Eagen, William J, Greenlee, Yan, Lin, Hsingan, Tsai, Yan, Xia, Ho-Sam, Ahn, Jacqueline, Agans-Fantuzzi, George, Boykow, Madhu, Chintala, Carolyn, Foster, Matthew, Bryant, Janice, Lau   +15 more
openaire   +2 more sources

An intronic polymorphism in the PAR-1 gene is associated with platelet receptor density and the response to SFLLRN

Blood, 2003
Protease-activated receptor 1 (PAR-1), the main thrombin receptor on vascular cells, plays a key role in platelet activation. We examined the range of PAR-1 expression on platelets, obtained twice, 1 week apart, from 100 healthy subjects and found a 2-fold interindividual variation in receptor numbers (95% CI = 858-1700).
Annabelle, Dupont, Pierre, Fontana, Christilla, Bachelot-Loza, Jean-Luc, Reny, Ivan, Biéche, Florence, Desvard, Martine, Aiach, Pascale, Gaussem   +7 more
openaire   +2 more sources