about
High throughput mutagenesis for identification of residues regulating human prostacyclin (hIP) receptor expression and functionμ-opioid receptors: correlation of agonist efficacy for signalling with ability to activate internalization.Fevipiprant (QAW039), a Slowly Dissociating CRTh2 Antagonist with the Potential for Improved Clinical Efficacy.The discovery of potent, orally bioavailable pyrazolo and triazolopyrimidine CXCR2 receptor antagonists.The discovery of potent, orally bioavailable pyrimidine-5-carbonitrile-6-alkyl CXCR2 receptor antagonists.Endomorphin-2: a biased agonist at the μ-opioid receptor.The role of kinetic context in apparent biased agonism at GPCRs.The antiallergic mast cell stabilizers lodoxamide and bufrolin as the first high and equipotent agonists of human and rat GPR35The long-acting beta-adrenoceptor agonist, indacaterol, inhibits IgE-dependent responses of human lung mast cells.Agonist efficacy and receptor desensitization: from partial truths to a fuller picture.Elusive equilibrium: the challenge of interpreting receptor pharmacology using calcium assays.PPARgamma is not a critical mediator of primary monocyte differentiation or foam cell formation.Long Receptor Residence Time of C26 Contributes to Super Agonist Activity at the Human β2 Adrenoceptor.Analysis of multiple histamine H₄ receptor compound classes uncovers Gαi protein- and β-arrestin2-biased ligands.Agonist-biased signaling at the histamine H4 receptor: JNJ7777120 recruits β-arrestin without activating G proteins.Efficacy is a contributing factor to the clinical onset of bronchodilation of inhaled beta(2)-adrenoceptor agonists.Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding.'Partial' competition of heterobivalent ligand binding may be mistaken for allosteric interactions: a comparison of different target interaction models.A single point mutation (N514Y) in the human M3 muscarinic acetylcholine receptor reveals differences in the properties of antagonists: evidence for differential inverse agonism.Simulating the influence of plasma protein on measured receptor affinity in biochemical assays reveals the utility of Schild analysis for estimating compound affinity for plasma proteins.BJP issue on drug discovery.Potent and efficacious inhibition of CXCR2 signaling by biparatopic nanobodies combining two distinct modes of action.Extrapyramidal side effects of antipsychotics are linked to their association kinetics at dopamine D2 receptors.Reassessment of the pharmacology of Sphingosine-1-phosphate S1P3 receptor ligands using the DiscoveRx PathHunter™ and Ca2+ release functional assays.Quantifying the association and dissociation rates of unlabelled antagonists at the muscarinic M3 receptor.Enhancement of the response to purinergic agonists in P2Y1 transfected 1321N1 cells by antagonists suramin and PPADS.Investigating the molecular mechanisms through which FTY720-P causes persistent S1P1 receptor internalizationSlow receptor dissociation is not a key factor in the duration of action of inhaled long-acting β2-adrenoceptor agonistsComparing the cardiovascular therapeutic indices of glycopyrronium and tiotropium in an integrated rat pharmacokinetic, pharmacodynamic and safety model.An investigation into the structure-activity relationships associated with the systematic modification of the β(2)-adrenoceptor agonist indacaterol.Evidence that P2Y4 nucleotide receptors are involved in the regulation of rat aortic smooth muscle cells by UTP and ATP.Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists.The in vitro metabolism of sphingosine-1-phosphate: identification; inhibition and pharmacological implications.Exploring the mechanism of agonist efficacy: a relationship between efficacy and agonist dissociation rate at the muscarinic M3 receptor.The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting β2-adrenoceptor agonist.In vitro and in vivo pharmacological characterization of 5-[(R)-2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quinolin-2-one (indacaterol), a novel inhaled beta(2) adrenoceptor agonist with a 24-h duration of action.The Influence of receptor kinetics on the onset and duration of action and the therapeutic index of NVA237 and tiotropium.Micro-pharmacokinetics: Quantifying local drug concentration at live cell membranes.Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP2 Receptor Antagonist for Treatment of Asthma.An Alternative Thiol-Reactive Dye to Analyze Ligand Interactions with the Chemokine Receptor CXCR2 Using a New Thermal Shift Assay Format.
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P50
description
hulumtues
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onderzoeker
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researcher
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հետազոտող
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Steven J. Charlton
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Steven J. Charlton
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Steven J. Charlton
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Steven J. Charlton
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Steven J. Charlton
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Steven J. Charlton
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Steven J. Charlton
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Steven J. Charlton
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Steven J. Charlton
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Steven J. Charlton
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Steve Charlton
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Steven J Charlton
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Steven J. Charlton
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Steven J. Charlton
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Steven J. Charlton
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Steven J. Charlton
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Steven J. Charlton
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P106
P1153
35608817000
P21
P31
P496
0000-0001-8841-2752