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Generation and characterization of an antagonistic monoclonal antibody against an extracellular domain of mouse DP2 (CRTH2/GPR44) receptors for prostaglandin D2.
PLoS One
September 2017
International Institute for Integrative Sleep Medicine (WPI-IIIS), University of Tsukuba, Tsukuba, Japan.
Prostaglandin D2 (PGD2) is a lipid mediator involved in sleep regulation and inflammation. PGD2 interacts with 2 types of G protein-coupled receptors, DP1 and DP2/CRTH2 (chemoattractant receptor homologous molecule expressed on T helper type 2 cells)/GPR44 to show a variety of biological effects. DP1 activation leads to Gs-mediated elevation of the intracellular cAMP level, whereas activation of DP2 decreases this level via the Gi pathway; and it also induces G protein-independent, arrestin-mediated cellular responses.
View Article and Find Full Text PDFCRTH2 is not involved in the anti-enteropooling effect of PGD2 in the small intestine.
Pharmacology
April 2008
Institute of Experimental and Clinical Pharmacology, Medical University Graz, Graz, Austria.
The majority of prostaglandins (PGs) are known to induce intestinal fluid secretion (enteropooling). In contrast, PGD(2) has been demonstrated to inhibit fluid secretion induced by other PGs. This study was aimed to investigate, by the use of selective agonists/antagonists, which type of PGD(2) receptor mediates this inhibitory effect.
View Article and Find Full Text PDFAgonist and antagonist effects of 15R-prostaglandin (PG) D2 and 11-methylene-PGD2 on human eosinophils and basophils.
J Pharmacol Exp Ther
January 2007
Meakins-Christie Laboratories, Department of Medicine, McGill University, 3626 St. Urbain Street, Montreal, Quebec H2X 2P2, Canada.
Prostaglandin (PG) D2 acts through both the DP(1) receptor, which is coupled to adenylyl cyclase, and the DP2 receptor (chemoattractant receptor-homologous molecule expressed on Th2 cells), which is present on eosinophils, basophils, and Th2 cells and results in cell activation and migration. The most potent prostanoid DP2 agonist so far reported is 15R-methyl-PGD2, in which the hydroxyl group has the unnatural R configuration. In contrast, the corresponding analog possessing the natural 15S configuration is approximately 75 times less potent.
View Article and Find Full Text PDFSynthesis of 15R-PGD2: a potential DP2 receptor agonist.
Bioorg Med Chem Lett
April 2005
Claude Pepper Institute and Department of Chemistry, Florida Institute of Technology, 150 W. University Blvd., Melbourne, FL 32901, USA.
The first total synthesis of 15R-PGD(2)3 was accomplished. The approach used in this report is also an efficient method to produce 15R-PGE(2). 15R-PGD(2), a potential DP(2) receptor agonist, could be an important novel tool for defining the role of this receptor in inflammatory diseases.
View Article and Find Full Text PDF15R-methyl-prostaglandin D2 is a potent and selective CRTH2/DP2 receptor agonist in human eosinophils.
J Pharmacol Exp Ther
January 2003
Department of Medicine, Meakins-Christie Laboratories, McGill University, Montreal, Quebec, Canada.
Prostaglandin D2 (PGD2) is a mast cell-derived mediator that seems to play a role in asthma and allergic diseases. It is the only primary prostanoid to activate human eosinophils, which it accomplishes through the DP2 receptor/chemoattractant receptor-homologous molecule expressed on T helper cell type 2 (Th2) cells (CRTH2). In addition, PGD2 has both pro- and anti-inflammatory effects via the adenylyl cyclase-coupled DP1 receptor.
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