Protease Activated Receptor 1 Antagonists
Mostrando 1-8 de 8 artigos, teses e dissertações.
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1. Platelet protease-activated receptors expression and activity in patients with pulmonary arterial hypertension / Análise da expressão e atividade de receptores ativados por proteases em plaquetas de pacientes com hipertensão arterial pulmonar
A hipertensão arterial pulmonar é uma síndrome clínica e hemodinâmica, caracterizada pelo aumento de resistência vascular na microcirculação. A vasoconstrição presente na doença ocorre principalmente devido à disfunção endotelial, induzindo a um estado pró-trombótico onde a participação das plaquetas é inequívoca. A trombina, principal ag
Publicado em: 2009
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2. The protease-activated receptor-2 agonist induces gastric mucus secretion and mucosal cytoprotection
Protease-activated receptor-2 (PAR-2), a receptor activated by trypsin/tryptase, modulates smooth muscle tone and exocrine secretion in the salivary glands and pancreas. Given that PAR-2 is expressed throughout the gastrointestinal tract, we investigated effects of PAR-2 agonists on mucus secretion and gastric mucosal injury in the rat. PAR-2–activating pe
American Society for Clinical Investigation.
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3. Factor Xa as an interface between coagulation and inflammation. Molecular mimicry of factor Xa association with effector cell protease receptor-1 induces acute inflammation in vivo.
Coagulation proteases were tested in a rat model of acute inflammation. Subplantar injection of Factor Xa (10-30 microg) produced a time- and dose-dependent edema in the rat paw, and potentiated carrageenin-induced edema. In contrast, the homologous protease Factor IXa was ineffective. This inflammatory response was recapitulated by the Factor Xa sequence L8
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4. Activation and inhibition of G protein-coupled receptors by cell-penetrating membrane-tethered peptides
Classical ligands bind to the extracellular surface of their cognate receptors and activate signaling pathways without crossing the plasma membrane barrier. We selectively targeted the intracellular receptor–G protein interface by using cell-penetrating membrane-tethered peptides. Attachment of a palmitate group to peptides derived from the third intracell
The National Academy of Sciences.
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5. Design, synthesis, and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor
Protease-activated receptors (PARs) represent a unique family of seven-transmembrane G protein-coupled receptors, which are enzymatically cleaved to expose a truncated extracellular N terminus that acts as a tethered activating ligand. PAR-1 is cleaved and activated by the serine protease α-thrombin, is expressed in various tissues (e.g., platelets and vasc
The National Academy of Sciences.
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6. Bcl-2 and Fas/APO-1 regulate distinct pathways to lymphocyte apoptosis.
Activation of the cell surface receptor Fas/APO-1 (CD95) induces apoptosis in lymphocytes and regulates immune responses. The cytoplasmic membrane protein Bcl-2 inhibits lymphocyte killing by diverse cytotoxic agents, but we found it provided little protection against Fas/APO-1-transduced apoptosis in B lymphoid cell lines, thymocytes and activated T cells.
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7. Proliferative action of mast-cell tryptase is mediated by PAR2, COX2, prostaglandins, and PPARγ: Possible relevance to human fibrotic disorders
Mast-cell products can stimulate fibroblast proliferation, implying that these cells are key players in fibrosis. One mast-cell product, the serine protease tryptase, is known to activate protease-activated receptor 2 (PAR2) and cause proliferation of fibroblasts. We found that recombinant tryptase, human mast-cell (HMC-1) supernatant, which contains tryptas
National Academy of Sciences.
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8. Protease-activated receptors 1 and 4 mediate activation of human platelets by thrombin
Because of the role of thrombin and platelets in myocardial infarction and other pathological processes, identifying and blocking the receptors by which thrombin activates platelets has been an important goal. Three protease-activated receptors (PARs) for thrombin — PAR1, PAR3, and PAR4 — are now known. PAR1 functions in human platelets, and the recent o
American Society for Clinical Investigation.