Results 281 to 290 of about 410,064 (307)

Time course of recovery of endothelial cell surface thrombin receptor (PAR-1) expression

American Journal of Physiology-Cell Physiology, 1999
We studied dynamics of cell surface expression of proteolytically activated thrombin receptor (PAR-1) in human pulmonary artery endothelial cells (HPAEC). PAR-1 activation was measured by changes in cytosolic calcium concentration ([Ca2+]i) and HPAEC retraction response (determined by real-time transendothelial monolayer electrical resistance).
C A, Ellis, C, Tiruppathi, R, Sandoval, W D, Niles, A B, Malik   +4 more
openaire   +2 more sources

Discovery of a nonpeptidic small molecule antagonist of the human platelet thrombin receptor (PAR-1)

Bioorganic & Medicinal Chemistry Letters, 2002
The synthesis and biological evaluation of a series of nonpeptidic small molecule antagonists of the human platelet thrombin receptor (PAR-1) are described. Optimization of the 5-amino-3-arylisoxazole lead resulted in an approximate 100-fold increase in potency.
Philippe G, Nantermet, James C, Barrow, George F, Lundell, Janetta M, Pellicore, Kenneth E, Rittle, MaryBeth, Young, Roger M, Freidinger, Thomas M, Connolly, Cindra, Condra, Jerzy, Karczewski, Rodney A, Bednar, Stanley L, Gaul, Robert J, Gould, Kris, Prendergast, Harold G, Selnick   +14 more
openaire   +2 more sources

Non-Peptidic Small-Molecule Antagonists of the Human Platelet Thrombin Receptor PAR-1

Current Medicinal Chemistry-Cardiovascular & Hematological Agents, 2003
The thrombin receptor on human platelets is the first member identified of a new family of G-protein coupled receptors referred to as protease activated receptors (PARs). These receptors are activated by a unique mechanism involving proteolytic cleavage of a portion of the extracellular domain to generate a new N-terminus which then acts as a tethered ...
H G, Selnick, J C, Barrow, P G, Nantermet, T M, Connolly   +3 more
openaire   +2 more sources

Activation of rat mast cells upon stimulation of protease-activated receptor (PAR-1)

Bulletin of Experimental Biology and Medicine, 2000
In vivo experiments on the model of wound healing showed that thrombin and thrombin receptor agonist TRAP-6 stimulated heparin secretion by mast cells in rat subcutaneous fat: the saturation of mast cells with heparin decreased, while degranulation and granulolysis increased.
B A, Umarova, T N, Dugina, E V, Shestakova, E, Gluza, S M, Strukova   +4 more
openaire   +2 more sources

Investigation of PAR-1-type thrombin receptors in rat glioma C6 cells with a novel monoclonal anti-PAR-1 antibody (Mab COR7-6H9)

Journal of Neurocytology, 1998
Rat glioma C6 cells have been demonstrated to be a suitable model in the investigation of PAR-1-type thrombin receptors in brain. However, anti-PAR-1 antibodies, which should be very helpful tools in studying PAR-1 in rat cells, have not been available up until now.
R, Kaufmann, B, Bone, M, Westermann, G, Nowak, V, Ramakrishnan   +4 more
openaire   +2 more sources

Receptor Binding and Agonist Efficacy: New Insights from Mutants of the Thrombin Protease-Activated Receptor-1 (PAR-1)

Molecular Pharmacology, 2000
The article by [Blackhart et al. (2000)][1], describing the differential activation of mutated thrombin protease-activated receptor-1 (PAR-1) either by the proteolytically revealed tethered ligand or by soluble receptor-activating peptides, adds yet another challenge to the theoretical ...
openaire   +2 more sources

Principles of PAR polarity in Caenorhabditis elegans embryos

Nature Reviews Molecular Cell Biology, 2013
Carsten Hoege, Anthony A Hyman, Hyman Anthony A   +2 more
exaly  

The Par-3 NTD adopts a PB1-like structure required for Par-3 oligomerization and membrane localization

EMBO Journal, 2007
Mingjie Zhang
exaly  

aPKC Cycles between Functionally Distinct PAR Protein Assemblies to Drive Cell Polarity

Developmental Cell, 2017
Josana Rodríguez, Florent Peglion, Lars Hubatsch   +2 more
exaly  

SCH-530348, a thrombin receptor (PAR-1) antagonist for the prevention and treatment of atherothrombosis.

Current opinion in investigational drugs (London, England : 2000), 2009
SCH-530348 is a novel antiplatelet agent undergoing development by Schering-Plough Corp for the treatment and prevention of atherothrombosis. The compound is an orally administered himbacine analog that potently antagonizes the platelet thrombin receptor protease-activated receptor 1 (PAR-1), which leaves the procoagulant function of thrombin intact ...
openaire   +1 more source