Results 261 to 270 of about 410,064 (307)
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Proteinase-activated receptor 1 (PAR-1) and cell apoptosis
Apoptosis, 2004This review summarizes the main aspects and newest findings of how proteinase-activated receptor 1 (PAR-1) may modulate programmed cell death. Activation of PAR-1 has been found to induce or inhibit apoptosis in a variety of cells, depending on the dosage of its physiological agonist thrombin, or that of synthetic receptor activators. To date, cellular
A N, Flynn, A G, Buret
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Pharmacological characterization of protease-activated receptor (PAR-1) in rat astrocytes
European Journal of Pharmacology, 1997The proteolytic action of thrombin on its receptor (protease-activated receptor-1 or PAR-1) results in a conformational change in which the new N-terminal sequence auto-activates the receptor. Peptide analogs of this N-terminal sequence (TRAPs) are able to mimic the effect of thrombin and an extensive search has led to the definition of the structural ...
T, Debeir, X, Vigé, J, Benavides
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Thrombin Receptor Antagonists, Recent Advances in PAR-1 Antagonist Development
Current Medicinal Chemistry, 2002The receptor for the serine protease thrombin, the protease-activated receptor-1 (PAR-1), has been recently characterized. Its key roles in thrombin-stimulated human platelet activation, vascular endothelial and smooth muscle proliferation, inflammatory responses and neurodegeneration suggest receptor involvement in various disorders such as arterial ...
M, Anderluh, M Sollner, Dolenc
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Peptide-Derived Protease-Activated Receptor-1 (PAR-1) Antagonists
Current Medicinal Chemistry-Cardiovascular & Hematological Agents, 2003Protease activated receptor-1 (PAR-1) is a G-coupled receptor cleaved by thrombin and other proteases to expose a new N-terminus, a "tethered ligand", that activates the receptor. Independently of proteolytic cleavage, peptides similar to the new N-terminus also activate the receptor, and structure activity relationships for the activating peptides ...
Steven M, Seiler, Michael S, Bernatowicz
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Macrocyclic hexapeptide analogues of the thrombin receptor (PAR-1) activation motif SFLLRN
Bioorganic & Medicinal Chemistry Letters, 1999The thrombin receptor (PAR-1) is activated by alpha-thrombin to stimulate various cell types, including platelets, through the tethered-ligand sequence SFLLRN. Macrocyclic peptide analogues of SFLLRN were synthesized and evaluated in vitro. In general, the compounds were much less potent in inducing platelet aggregation relative to SFLLRN-NH2 and did ...
D F, McComsey +4 more
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MOLECULAR MODELING OF PAR-1 COMPLEXES OF HUMAN RECEPTORS WITH THE VORAPAXAR MOLECULE
SAKHAROV READINGS 2021: ENVIRONMENTAL PROBLEMS OF THE XXI CENTURY Part 1, 2021Vorapaxar (SCH 530348) is a synthetic analogue of the natural substance himbacin, the first representative of a new class of antiplatelet antagonists of the protease-activated receptor (PAR-1) of thrombin.
A. D. Sinyak, A. V. Bakunovich
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Distribution and potential biologic function of the thrombin receptor PAR-1 on human keratinocytes
Archives of Dermatological Research, 2000Thrombin has recently been shown not only to exert procoagulant activities, but also to induce mitogenic responses of different cell types involved in wound healing via binding to and cleavage of the thrombin receptor. In order to further explore these aspects of thrombin function, human keratinocytes (HaCaT cell line) were examined for their potential
B, Algermissen +5 more
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Expression of the thrombin receptor (PAR‐1) during rat skeletal muscle differentiation
Journal of Cellular Physiology, 2001AbstractThe serine protease thrombin has been proposed to be involved in neuromuscular plasticity. Its specific receptor “protease activated receptor‐1” (PAR‐1), a G protein‐coupled receptor, has been shown to be expressed in myoblasts but not after fusion (Suidan et al., 1996 J Biol Chem 271:29162–29169).
F, Chevessier +2 more
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Himbacine derived thrombin receptor (PAR-1) antagonists: SAR of the pyridine ring
Bioorganic & Medicinal Chemistry Letters, 2007The structure-activity relationship (SAR) of the vinyl pyridine region of himbacine derived thrombin receptor (PAR-1) antagonists is described. A 2-vinylpyridyl ring substituted with an aryl or a heteroaryl group at the 5-position showed the best overall PAR-1 affinity and pharmacokinetic properties.
Yan, Xia +12 more
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Vorapaxar, an oral PAR‐1 receptor antagonist, does not affect the pharmacokinetics of rosiglitazone
Clinical Pharmacology in Drug Development, 2014AbstractPurposeTo evaluate the potential effects of vorapaxar on the pharmacokinetics and safety of rosiglitazone.MethodsThis was an open‐label, two‐period, two‐treatment, fixed‐sequence study in 18 healthy subjects. On Day 1, Period 1, subjects received a single dose of rosiglitazone 8 mg.
Teddy, Kosoglou +7 more
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