Search Results - "Charlton, SJ"

A common intracellular allosteric binding site for antagonists of the CXCR2 receptor by Salchow, K, Bond, ME, Evans, SC, Press, NJ, Charlton, SJ, Hunt, PA, Bradley, ME

“…Background and purpose:  We have previously shown that SB265610 (1‐(2‐bromo‐phenyl)‐3‐(7‐cyano‐3H‐benzotriazol‐4‐yl)‐urea) behaves as an allosteric, inverse…”
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SB265610 is an allosteric, inverse agonist at the human CXCR2 receptor by Bradley, ME, Bond, ME, Manini, J, Brown, Z, Charlton, SJ

“…Background and purpose:  In several previous studies, the C‐X‐C chemokine receptor (CXCR)2 antagonist 1‐(2‐bromo‐phenyl)‐3‐(7‐cyano‐3H‐benzotriazol‐4‐yl)‐urea…”
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Reassessment of the pharmacology of Sphingosine‐1‐phosphate S1P3 receptor ligands using the DiscoveRx PathHunter™ and Ca2+ release functional assays by Riddy, DM, Stamp, C, Sykes, DA, Charlton, SJ, Dowling, MR

“…BACKGROUND AND PURPOSE DiscoverRx's PathHunter™ assay measures GPCR agonist potency, via the recruitment of β‐arrestin, independent of the subtype of Gα…”
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Pharmacogenetic characterization of indacaterol, a novel β2‐adrenoceptor agonist by Sayers, I, Hawley, J, Stewart, CE, Billington, CK, Henry, A, Leighton‐Davies, JR, Charlton, SJ, Hall, IP

“…Background and purpose: Indacaterol is a novel β2‐adrenoceptor agonist in development for the treatment of chronic obstructive pulmonary disease. The aim of…”
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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 by Battram, Cliff, Charlton, Steven J, Cuenoud, Bernard, Dowling, Mark R, Fairhurst, Robin A, Farr, David, Fozard, John R, Leighton-Davies, Juliet R, Lewis, Christine A, McEvoy, Lorraine, Turner, Robert J, Trifilieff, Alexandre

“…Here, we describe the preclinical pharmacological profile of 5-[(R)-2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quinolin-2-one (indacaterol),…”
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Airway remodeling disease: primary human structural cells and phenotypic and pathway assays to identify targets with potential to prevent or reverse remodeling by Rosethorne, Elizabeth M, Charlton, Steven J

“…Airway remodeling is a characteristic of many chronic respiratory diseases and occurs when there are significant changes to the architecture of the small and…”
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Reassessment of the pharmacology of Sphingosine‐1‐phosphate S1P 3 receptor ligands using the DiscoveRx PathHunter™ and Ca 2+ release functional assays by Riddy, DM, Stamp, C, Sykes, DA, Charlton, SJ, Dowling, MR

“…BACKGROUND AND PURPOSE DiscoverRx's PathHunter™ assay measures GPCR agonist potency, via the recruitment of β‐arrestin, independent of the subtype of G α…”
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Pharmacogenetic characterization of indacaterol, a novel beta 2-adrenoceptor agonist by Sayers, I, Hawley, J, Stewart, C E, Billington, C K, Henry, A, Leighton-Davies, J R, Charlton, S J, Hall, I P

“…Indacaterol is a novel beta(2)-adrenoceptor agonist in development for the treatment of chronic obstructive pulmonary disease. The aim of this study was to…”
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PPADS and suramin as antagonists at cloned P 2Y ‐ and P 2U ‐purinoceptors by Charlton, Steven J., Brown, Colin A., Weisman, Gary A., Turner, John T., Erb, Laurie, Boarder, Michael R.

“…The effect of suramin and pyridoxalphosphate‐6‐azophenyl‐2′,4′‐disulphonic acid (PPADS) on the stimulation of phospholipase C in 1321N1 cells transfected with…”
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EXPRESSION AND FUNCTIONAL ANALYSIS OF CHEMOKINE RECEPTORS IN HUMAN PERIPHERAL BLOOD LEUKOCYTE POPULATIONS by Patel, L., Charlton, S.J., Chambers, J.K., Macphee, C.H.

“…Emerging evidence indicates that chemokine receptor expression patterns are critical in determining the spectrum of action of the chemokines. We have analysed…”
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Assessing the minimum number of data points required for accurate IC50 determination by Turner, Robert J, Charlton, Steven J

“…Combinatorial chemistry technology has enabled the synthesis of large, targeted libraries consisting of a much higher ratio of pharmacologically active…”
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PPADS and suramin as antagonists at cloned P2Y‐ and P2U‐purinoceptors by Charlton, Steven J., Brown, Colin A., Weisman, Gary A., Turner, John T., Erb, Laurie, Boarder, Michael R.

“…1 The effect of suramin and pyridoxalphosphate‐6‐azophenyl‐2′,4′‐disulphonic acid (PPADS) on the stimulation of phospholipase C in 1321N1 cells transfected…”
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Cloned and transfected P2Y4 receptors: characterization of a suramin and PPADS‐insensitive response to UTP by Charlton, Steven J., Brown, Colin A., Weisman, Gary A., Turner, John T., Erb, Laurie, Boarder, Michael R.

“…The P2Y family of receptors are G protein‐coupled receptors for ATP, ADP, UTP and UDP. Recently several members of this family have been cloned, including the…”
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PPARγ Is Not a Critical Mediator of Primary Monocyte Differentiation or Foam Cell Formation by Patel, Lisa, Charlton, Steven J., Marshall, Ian C., Moore, Gary B.T., Coxon, Phil, Moores, Kitty, Clapham, John C., Newman, Suzanna J., Smith, Stephen A., Macphee, Colin H.

“…In the present report we clarify the role of PPARγ in differentiation and function of human-derived monocyte/macrophages in vitro. Rosiglitazone, a selective…”
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ATP priming of macrophage-derived chemokine responses in CHO cells expressing the CCR4 receptor by Rosethorne, Elizabeth M, Leighton-Davies, Juliet R, Beer, David, Charlton, Steven J

“…The mechanism by which ATP primes for subsequent macrophage-derived chemokine (MDC) mediated intracellular calcium (Ca2+(i)) responses at the human CCR4…”
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Responses of the longitudinal muscle and the muscularis mucosae of the rat duodenum to adenine and uracil nucleotides by Johnson, C.R., Charlton, S.J., Hourani, S.M.O.

“…1 Previous studies have shown that the rat duodenum contains P1 and P2Y purinoceptors via which it relaxes to adenosine and adenosine 5′‐triphosphate (ATP)…”
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Initial development of a predictive hydrocarbon emissions model for a DI diesel engine by Carter, S.J., Hawley, J.G., Slowley, J., Charlton, S.J.

“…The drive towards lower emissions from automotive diesel engines as a consequence of strict environmental regulations has resulted in extensive R&D programmes…”
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