A5074907384- Inflammatory mediators and NSAID effects
- Receptor Mechanisms and Signaling
- Asthma and respiratory diseases
- Mycorrhizal Fungi and Plant Interactions
- Advanced MIMO Systems Optimization
- Fungal Biology and Applications
- Neuropeptides and Animal Physiology
- Estrogen and related hormone effects
- IoT and Edge/Fog Computing
- Eicosanoids and Hypertension Pharmacology
- Synthesis and Biological Evaluation
- Drug Transport and Resistance Mechanisms
- Chemokine receptors and signaling
- Chemical Synthesis and Analysis
- Cannabis and Cannabinoid Research
- Lichen and fungal ecology
- Synthesis of Organic Compounds
- Nitric Oxide and Endothelin Effects
- Cooperative Communication and Network Coding
- ICT Impact and Policies
- Advanced Wireless Network Optimization
- Plant Pathogens and Fungal Diseases
- Coagulation, Bradykinin, Polyphosphates, and Angioedema
- Animal Virus Infections Studies
- Mast cells and histamine
Commonwealth Scientific and Industrial Research Organisation
2017-2019
Data61
2016-2019
Australian National University
2016-2017
Douglass Hanly Moir Pathology
2016
Institute for Research in Immunology and Cancer
2013
Université de Montréal
2013
Merck Canada Inc. (Canada)
2000-2011
TransCanada (Canada)
2006-2011
Merck (Japan)
1997-2010
The University of Sydney
2005-2006
A cDNA encoding a functional human prostanoid DP (hDP) receptor has been constructed from genomic clone and fragment cloned by 3′-rapid amplification of ends-polymerase chain reaction. The hDP consists 359 amino acid residues with predicted molecular mass 40,276 the putative heptahelical transmembrane domains characteristic G-protein-coupled receptors. deduced sequence receptor, when compared all other members family, shows highest degree identity hIP hEP2 receptors, followed hEP4 receptor....
A cDNA clone encoding the human prostaglandin (PG) E2 receptor EP2 subtype has been isolated from a lung library. The 1.9-kilobase pair cDNA, hEP2, encodes for 488-amino acid protein with predicted molecular mass of 53,115 and seven putative transmembrane domains characteristic G protein-coupled receptors. specific binding [3H]PGE2 to COS cell membranes transfected hEP2 was high affinity an equilibrium dissociation constant (Kd) 1 nM rank order potency prostaglandins in competition PGE1 =...
1. The recombinant human prostaglandin D(2) (PGD(2)) receptor, hCRTH2, has been expressed in HEK293(EBNA) and characterized with respect to radioligand binding signal transduction properties. High low affinity sites for PGD(2) were identified the CRTH2 receptor population by saturation analysis respective equilibrium dissociation constants (K(D)) of 2.5 109 nM. This revealed that is eight times less than its DP receptor. 2. Equilibrium competition assays compounds tested, only several...
The discovery of the potent and selective prostaglandin D2 (PGD2) receptor (DP) antagonist [(3R)-4-(4-chlorobenzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (13) is presented. Initial lead antagonists 6 7 were found to be DP (DP Ki = 2.0 nM for each); however, they both suffered from poor pharmacokinetic profiles, short half-lives high clearance rates in rats. Rat bile duct cannulation studies revealed that concentrations parent drug present biliary...
Prostaglandin (PG) E(2) is a potent inducer of cortical and trabecular bone formation in humans animals. Although the anabolic action PGE(2) well documented, cellular molecular mechanisms that mediate this effect remain unclear. This study was undertaken to examine pharmacological inactivation prostanoid receptor EP(4), one receptors, on PGE(2)-induced vivo. We first determined ability EP(4)A, an EP(4)-selective ligand, act as antagonist. increases intracellular cAMP suppresses apoptosis...
In underlaid device-to-device (D2D) cellular networks, severe radio interference can be typical for and D2D users, which causes each user's quality-of-experience (QoE) to degrade significantly. Thus, in this paper, a dynamic Stackelberg game is formulated with single-leader (base station) multiple-followers (D2D pairs). The leader reduces within the network by charging price followers, whereas followers react compete find optimal transmit power resource block allocation. To enhance user QoE,...
The chemoattractant receptor-homologous molecule expressed on T-helper type 2 cells (CRTH2) is a G protein-coupled receptor that has been reported to modulate inflammatory responses in various rodent models of asthma, allergic rhinitis and atopic dermatitis. In this study, we describe the biological pharmacological properties {(7R)-7-[[(4-fluorophenyl)sulfonyl](methyl)amino]-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl}acetic acid (MK-7246), novel synthetic CRTH2 antagonist. We show MK-7246 1)...
A 4-year-old girl and a 4-month-old boy presented with hypoglycemia, normal electrolytes, low cortisol, high ACTH. diagnosis of primary adrenal insufficiency was made initial treatment glucocorticoids mineralocorticoids. The genes known to cause ACTH resistance were normal. Whole exome sequencing revealed that the compound heterozygous for POMC mutations: one previously described null allele novel p.R8C mutation in sequence encoding α-MSH. homozygous mutation. mutant is immunoreactive, but...
The size and distribution of Cortinarius rotundisporus genets at three sclerophyll forest field sites in New South Wales, Australia, were estimated by using microsatellite‐primed PCR (MS‐PCR) DNA extracted from sporocarp tissue. MS‐PCR fingerprints generated with the primers (GTG) 5 (GACA) 4 indicated that two to five present each site, site being characterized a single large genet (9–30 m diameter). Analysis internal transcribed spacer (ITS)‐RFLP patterns individual sporocarps used study...
The structure-activity relationship (SAR) of prostaglandin (PG) E(2) at the human EP(1) prostanoid receptor (designated hEP(1)) was examined via binding and activation this by a series 55 prostanoids analogs. Using clonal embryonic kidney 293 cell lines expressing recombinant hEP(1), affinity (K(i)), potency (EC(50)), efficacy data were obtained using radioligand competitive assay an aequorin-based calcium functional assay. All compounds behaved as full agonists (90-100% response elicited...
Abstract Objective —To evaluate whether the leukotriene (LT) D4 receptor antagonist L-708,738 is therapeutically beneficial in treating horses with recurrent airway obstruction (heaves). Animals —12 adult heaves and healthy lung lobes from 20 slaughtered horses. Procedure —Lung were used for smooth muscle tension radioligand binding studies. Horses given a placebo 14 days administered (n = 6; 2.5 mg/kg PO, q 12 h) or dexamethasone (6; 0.04 mg/kg, IV, 24 to 28. Pulmonary function was measured...
The chemoattractant receptor-homologous molecule expressed on T-helper type 2 cells (CRTH2) is a G protein-coupled receptor whose function in vivo has been incompletely characterized. One of the reasons that its current known ligands, prostaglandin D<sub>2</sub> and some metabolites, have either poor selectivity for CRTH2 or are metabolically unstable vivo. In this study, we describe biological pharmacological properties L-888,607, first synthetic potent selective agonist. We show L-888,607...