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Structure-Kinetic Profiling of Haloperidol Analogues at the Human Dopamine D2 Receptor.

Fyfe TJ, Kellam B, Sykes DA, Capuano B, Scammells PJ, Lane JR, Charlton SJ, Mistry SN.

J Med Chem. 2019 Oct 3. doi: 10.1021/acs.jmedchem.9b00864. [Epub ahead of print]


Pharmacological Characterization of a Novel 5-Hydroxybenzothiazolone-Derived β 2-Adrenoceptor Agonist with Functional Selectivity for Anabolic Effects on Skeletal Muscle Resulting in a Wider Cardiovascular Safety Window in Preclinical Studies.

Koziczak-Holbro M, Rigel DF, Dumotier B, Sykes DA, Tsao J, Nguyen NH, Bösch J, Jourdain M, Flotte L, Adachi Y, Kiffe M, Azria M, Fairhurst RA, Charlton SJ, Richardson BP, Lach-Trifilieff E, Glass DJ, Ullrich T, Hatakeyama S.

J Pharmacol Exp Ther. 2019 May;369(2):188-199. doi: 10.1124/jpet.118.255307. Epub 2019 Feb 28.


Airway remodeling disease: primary human structural cells and phenotypic and pathway assays to identify targets with potential to prevent or reverse remodeling.

Rosethorne EM, Charlton SJ.

J Exp Pharmacol. 2018 Nov 29;10:75-85. doi: 10.2147/JEP.S159124. eCollection 2018. Review.


Preassembled GPCR signaling complexes mediate distinct cellular responses to ultralow ligand concentrations.

Civciristov S, Ellisdon AM, Suderman R, Pon CK, Evans BA, Kleifeld O, Charlton SJ, Hlavacek WS, Canals M, Halls ML.

Sci Signal. 2018 Oct 9;11(551). pii: eaan1188. doi: 10.1126/scisignal.aan1188.


Reply to 'Antipsychotics with similar association kinetics at dopamine D2 receptors differ in extrapyramidal side-effects'.

Sykes DA, Lane JR, Szabo M, Capuano B, Javitch JA, Charlton SJ.

Nat Commun. 2018 Sep 3;9(1):3568. doi: 10.1038/s41467-018-05678-4. No abstract available.


Single Step Determination of Unlabeled Compound Kinetics Using a Competition Association Binding Method Employing Time-Resolved FRET.

Sykes DA, Charlton SJ.

Methods Mol Biol. 2018;1824:177-194. doi: 10.1007/978-1-4939-8630-9_10.


The inhibition of human lung fibroblast proliferation and differentiation by Gs-coupled receptors is not predicted by the magnitude of cAMP response.

Roberts MJ, Broome RE, Kent TC, Charlton SJ, Rosethorne EM.

Respir Res. 2018 Apr 7;19(1):56. doi: 10.1186/s12931-018-0759-2.


Micro-pharmacokinetics: Quantifying local drug concentration at live cell membranes.

Gherbi K, Briddon SJ, Charlton SJ.

Sci Rep. 2018 Feb 22;8(1):3479. doi: 10.1038/s41598-018-21100-x.


Strong Heterogeneity in Advances in Cryopreservation Techniques in the Mammalian Orders.

Charlton SJ, Nielsen MB, Pedersen CR, Thomsen L, Kristjansen MP, Sørensen TB, Pertoldi C, Strand J.

Zoolog Sci. 2018 Feb;35(1):1-22. doi: 10.2108/zs170037. Review.


Biased Agonism in Drug Discovery-Is It Too Soon to Choose a Path?

Michel MC, Charlton SJ.

Mol Pharmacol. 2018 Apr;93(4):259-265. doi: 10.1124/mol.117.110890. Epub 2018 Jan 11. Review.


Extrapyramidal side effects of antipsychotics are linked to their association kinetics at dopamine D2 receptors.

Sykes DA, Moore H, Stott L, Holliday N, Javitch JA, Lane JR, Charlton SJ.

Nat Commun. 2017 Oct 2;8(1):763. doi: 10.1038/s41467-017-00716-z.


Correction to "Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP2 Receptor Antagonist for Treatment of Asthma".

Sandham DA, Barker L, Brown L, Brown Z, Budd D, Charlton SJ, Chatterjee D, Cox B, Dubois G, Duggan N, Hall E, Hatto J, Leblanc C, Maas J, Manini J, Profit R, Riddy D, Ritchie C, Sohal B, Shaw D, Stringer R, Sykes DA, Thomas M, Turner KL, Watson SJ, West R, Willard E, Williams G, Willis J.

ACS Med Chem Lett. 2017 Sep 1;8(9):987. doi: 10.1021/acsmedchemlett.7b00353. eCollection 2017 Sep 14.


Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP2 Receptor Antagonist for Treatment of Asthma.

Sandham DA, Barker L, Brown L, Brown Z, Budd D, Charlton SJ, Chatterjee D, Cox B, Dubois G, Duggan N, Hall E, Hatto J, Maas J, Manini J, Profit R, Riddy D, Ritchie C, Sohal B, Shaw D, Stringer R, Sykes DA, Thomas M, Turner KL, Watson SJ, West R, Willard E, Williams G, Willis J.

ACS Med Chem Lett. 2017 Apr 25;8(5):582-586. doi: 10.1021/acsmedchemlett.7b00157. eCollection 2017 May 11. Erratum in: ACS Med Chem Lett. 2017 Sep 01;8(9):987.


Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding.

Dickson CJ, Hornak V, Velez-Vega C, McKay DJ, Reilly J, Sandham DA, Shaw D, Fairhurst RA, Charlton SJ, Sykes DA, Pearlstein RA, Duca JS.

J Med Chem. 2016 Jun 23;59(12):5780-9. doi: 10.1021/acs.jmedchem.6b00358. Epub 2016 Jun 7.


Fevipiprant (QAW039), a Slowly Dissociating CRTh2 Antagonist with the Potential for Improved Clinical Efficacy.

Sykes DA, Bradley ME, Riddy DM, Willard E, Reilly J, Miah A, Bauer C, Watson SJ, Sandham DA, Dubois G, Charlton SJ.

Mol Pharmacol. 2016 May;89(5):593-605. doi: 10.1124/mol.115.101832. Epub 2016 Feb 25.


The role of kinetic context in apparent biased agonism at GPCRs.

Klein Herenbrink C, Sykes DA, Donthamsetti P, Canals M, Coudrat T, Shonberg J, Scammells PJ, Capuano B, Sexton PM, Charlton SJ, Javitch JA, Christopoulos A, Lane JR.

Nat Commun. 2016 Feb 24;7:10842. doi: 10.1038/ncomms10842.


Long Receptor Residence Time of C26 Contributes to Super Agonist Activity at the Human β2 Adrenoceptor.

Rosethorne EM, Bradley ME, Gherbi K, Sykes DA, Sattikar A, Wright JD, Renard E, Trifilieff A, Fairhurst RA, Charlton SJ.

Mol Pharmacol. 2016 Apr;89(4):467-75. doi: 10.1124/mol.115.101253. Epub 2016 Jan 15.


An Alternative Thiol-Reactive Dye to Analyze Ligand Interactions with the Chemokine Receptor CXCR2 Using a New Thermal Shift Assay Format.

Bergsdorf C, Fiez-Vandal C, Sykes DA, Bernet P, Aussenac S, Charlton SJ, Schopfer U, Ottl J, Duckely M.

J Biomol Screen. 2016 Mar;21(3):243-51. doi: 10.1177/1087057115619597. Epub 2015 Dec 7.


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.

Blakeley D, Sykes DA, Ensor P, Bertran E, Aston PJ, Charlton SJ.

Br J Pharmacol. 2015 Nov;172(21):5037-49. doi: 10.1111/bph.13263. Epub 2015 Oct 22.


Comparing the cardiovascular therapeutic indices of glycopyrronium and tiotropium in an integrated rat pharmacokinetic, pharmacodynamic and safety model.

Trifilieff A, Ethell BT, Sykes DA, Watson KJ, Collingwood S, Charlton SJ, Kent TC.

Toxicol Appl Pharmacol. 2015 Aug 15;287(1):9-16. doi: 10.1016/j.taap.2015.05.012. Epub 2015 May 27.


Functional desensitization of the β 2 adrenoceptor is not dependent on agonist efficacy.

Rosethorne EM, Bradley ME, Kent TC, Charlton SJ.

Pharmacol Res Perspect. 2015 Feb;3(1):e00101. doi: 10.1002/prp2.101. Epub 2015 Jan 5.


'Partial' competition of heterobivalent ligand binding may be mistaken for allosteric interactions: a comparison of different target interaction models.

Vauquelin G, Hall D, Charlton SJ.

Br J Pharmacol. 2015 May;172(9):2300-15. doi: 10.1111/bph.13053. Epub 2015 Mar 17.


Potent and efficacious inhibition of CXCR2 signaling by biparatopic nanobodies combining two distinct modes of action.

Bradley ME, Dombrecht B, Manini J, Willis J, Vlerick D, De Taeye S, Van den Heede K, Roobrouck A, Grot E, Kent TC, Laeremans T, Steffensen S, Van Heeke G, Brown Z, Charlton SJ, Cromie KD.

Mol Pharmacol. 2015 Feb;87(2):251-62. doi: 10.1124/mol.114.094821. Epub 2014 Dec 2.


The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting β2-adrenoceptor agonist.

Arnold N, Beattie D, Bradley M, Brearley A, Brown L, Charlton SJ, Fairhurst RA, Farr D, Fozard J, Fullerton J, Gosling M, Hatto J, Janus D, Jones D, Jordan L, Lewis C, Maas J, McCarthy C, Mercer M, Oakman H, Press N, Profit R, Schuerch F, Sykes D, Taylor RJ, Trifilieff A, Tuffnell A.

Bioorg Med Chem Lett. 2014 Sep 1;24(17):4341-7. doi: 10.1016/j.bmcl.2014.06.014. Epub 2014 Jun 26.


The discovery of potent, orally bioavailable pyrimidine-5-carbonitrile-6-alkyl CXCR2 receptor antagonists.

Porter DW, Bradley M, Brown Z, Charlton SJ, Cox B, Hunt P, Janus D, Lewis S, Oakley P, O'Connor D, Reilly J, Smith N, Press NJ.

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3285-90. doi: 10.1016/j.bmcl.2014.06.011. Epub 2014 Jun 14.


High throughput mutagenesis for identification of residues regulating human prostacyclin (hIP) receptor expression and function.

Bill A, Rosethorne EM, Kent TC, Fawcett L, Burchell L, van Diepen MT, Marelli A, Batalov S, Miraglia L, Orth AP, Renaud NA, Charlton SJ, Gosling M, Gaither LA, Groot-Kormelink PJ.

PLoS One. 2014 Jun 2;9(6):e97973. doi: 10.1371/journal.pone.0097973. eCollection 2014.


Identification of novel IP receptor agonists using historical ligand biased chemical arrays.

McKeown SC, Charlton SJ, Cox B, Fitch H, Howson CD, Leblanc C, Meyer A, Rosethorne EM, Stanley E.

Bioorg Med Chem Lett. 2014 May 15;24(10):2247-50. doi: 10.1016/j.bmcl.2014.03.089. Epub 2014 Apr 5.


The pharmacological rationale for combining muscarinic receptor antagonists and β-adrenoceptor agonists in the treatment of airway and bladder disease.

Dale PR, Cernecka H, Schmidt M, Dowling MR, Charlton SJ, Pieper MP, Michel MC.

Curr Opin Pharmacol. 2014 Jun;16:31-42. doi: 10.1016/j.coph.2014.03.003. Epub 2014 Mar 27. Review.


Investigating the molecular mechanisms through which FTY720-P causes persistent S1P1 receptor internalization.

Sykes DA, Riddy DM, Stamp C, Bradley ME, McGuiness N, Sattikar A, Guerini D, Rodrigues I, Glaenzel A, Dowling MR, Mullershausen F, Charlton SJ.

Br J Pharmacol. 2014 Nov;171(21):4797-807. doi: 10.1111/bph.12620.


Observed drug-receptor association rates are governed by membrane affinity: the importance of establishing "micro-pharmacokinetic/pharmacodynamic relationships" at the β2-adrenoceptor.

Sykes DA, Parry C, Reilly J, Wright P, Fairhurst RA, Charlton SJ.

Mol Pharmacol. 2014 Apr;85(4):608-17. doi: 10.1124/mol.113.090209. Epub 2014 Jan 29.


The antiallergic mast cell stabilizers lodoxamide and bufrolin as the first high and equipotent agonists of human and rat GPR35.

MacKenzie AE, Caltabiano G, Kent TC, Jenkins L, McCallum JE, Hudson BD, Nicklin SA, Fawcett L, Markwick R, Charlton SJ, Milligan G.

Mol Pharmacol. 2014 Jan;85(1):91-104. doi: 10.1124/mol.113.089482. Epub 2013 Oct 10.


Detailed analysis of biased histamine H₄ receptor signalling by JNJ 7777120 analogues.

Nijmeijer S, Vischer HF, Sirci F, Schultes S, Engelhardt H, de Graaf C, Rosethorne EM, Charlton SJ, Leurs R.

Br J Pharmacol. 2013 Sep;170(1):78-88. doi: 10.1111/bph.12117.


Analysis of multiple histamine H₄ receptor compound classes uncovers Gαi protein- and β-arrestin2-biased ligands.

Nijmeijer S, Vischer HF, Rosethorne EM, Charlton SJ, Leurs R.

Mol Pharmacol. 2012 Dec;82(6):1174-82. doi: 10.1124/mol.112.080911. Epub 2012 Sep 12.


An investigation into the structure-activity relationships associated with the systematic modification of the β(2)-adrenoceptor agonist indacaterol.

Beattie D, Beer D, Bradley ME, Bruce I, Charlton SJ, Cuenoud BM, Fairhurst RA, Farr D, Fozard JR, Janus D, Rosethorne EM, Sandham DA, Sykes DA, Trifilieff A, Turner KL, Wissler E.

Bioorg Med Chem Lett. 2012 Oct 1;22(19):6280-5. doi: 10.1016/j.bmcl.2012.07.096. Epub 2012 Aug 4.


The Influence of receptor kinetics on the onset and duration of action and the therapeutic index of NVA237 and tiotropium.

Sykes DA, Dowling MR, Leighton-Davies J, Kent TC, Fawcett L, Renard E, Trifilieff A, Charlton SJ.

J Pharmacol Exp Ther. 2012 Nov;343(2):520-8. doi: 10.1124/jpet.112.194456. Epub 2012 Aug 1.


Reassessment of the pharmacology of Sphingosine-1-phosphate S1P3 receptor ligands using the DiscoveRx PathHunter™ and Ca2+ release functional assays.

Riddy DM, Stamp C, Sykes DA, Charlton SJ, Dowling MR.

Br J Pharmacol. 2012 Oct;167(4):868-80. doi: 10.1111/j.1476-5381.2012.02032.x.


Endomorphin-2: a biased agonist at the μ-opioid receptor.

Rivero G, Llorente J, McPherson J, Cooke A, Mundell SJ, McArdle CA, Rosethorne EM, Charlton SJ, Krasel C, Bailey CP, Henderson G, Kelly E.

Mol Pharmacol. 2012 Aug;82(2):178-88. doi: 10.1124/mol.112.078659. Epub 2012 May 2.


HDL-like discs for assaying membrane proteins in drug discovery.

Fiez-Vandal C, Leder L, Freuler F, Sykes D, Charlton SJ, Siehler S, Schopfer U, Duckely M.

Biophys Chem. 2012 May;165-166:56-61. doi: 10.1016/j.bpc.2012.03.005. Epub 2012 Mar 19.


The in vitro metabolism of sphingosine-1-phosphate: identification; inhibition and pharmacological implications.

Bradley ME, McGuinness N, Williams G, Charlton SJ, Dowling MR.

Eur J Pharmacol. 2011 Dec 15;672(1-3):56-61. doi: 10.1016/j.ejphar.2011.09.178. Epub 2011 Sep 29.


Slow receptor dissociation is not a key factor in the duration of action of inhaled long-acting β2-adrenoceptor agonists.

Sykes DA, Charlton SJ.

Br J Pharmacol. 2012 Apr;165(8):2672-83. doi: 10.1111/j.1476-5381.2011.01639.x.


Agonist-biased signaling at the histamine H4 receptor: JNJ7777120 recruits β-arrestin without activating G proteins.

Rosethorne EM, Charlton SJ.

Mol Pharmacol. 2011 Apr;79(4):749-57. doi: 10.1124/mol.110.068395. Epub 2010 Dec 6.


M3-muscarinic receptor promotes insulin release via receptor phosphorylation/arrestin-dependent activation of protein kinase D1.

Kong KC, Butcher AJ, McWilliams P, Jones D, Wess J, Hamdan FF, Werry T, Rosethorne EM, Charlton SJ, Munson SE, Cragg HA, Smart AD, Tobin AB.

Proc Natl Acad Sci U S A. 2010 Dec 7;107(49):21181-6. doi: 10.1073/pnas.1011651107. Epub 2010 Nov 15.


Elusive equilibrium: the challenge of interpreting receptor pharmacology using calcium assays.

Charlton SJ, Vauquelin G.

Br J Pharmacol. 2010 Nov;161(6):1250-65. doi: 10.1111/j.1476-5381.2010.00863.x. Review.


BJP issue on drug discovery.

Charlton SJ, Bond RA.

Br J Pharmacol. 2010 Nov;161(6):1201-2. doi: 10.1111/j.1476-5381.2010.01028.x. No abstract available.


Long-lasting target binding and rebinding as mechanisms to prolong in vivo drug action.

Vauquelin G, Charlton SJ.

Br J Pharmacol. 2010 Oct;161(3):488-508. doi: 10.1111/j.1476-5381.2010.00936.x. Review.


Measuring receptor target coverage: a radioligand competition binding protocol for assessing the association and dissociation rates of unlabeled compounds.

Sykes DA, Dowling MR, Charlton SJ.

Curr Protoc Pharmacol. 2010 Sep;Chapter 9:Unit 9.14. doi: 10.1002/0471141755.ph0914s50.


Efficacy is a contributing factor to the clinical onset of bronchodilation of inhaled beta(2)-adrenoceptor agonists.

Rosethorne EM, Turner RJ, Fairhurst RA, Charlton SJ.

Naunyn Schmiedebergs Arch Pharmacol. 2010 Sep;382(3):255-63. doi: 10.1007/s00210-010-0533-6. Epub 2010 Aug 8.


A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of beta2-adrenoceptor agonists as inhaled long-acting bronchodilators.

Beattie D, Bradley M, Brearley A, Charlton SJ, Cuenoud BM, Fairhurst RA, Gedeck P, Gosling M, Janus D, Jones D, Lewis C, McCarthy C, Oakman H, Stringer R, Taylor RJ, Tuffnell A.

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5302-7. doi: 10.1016/j.bmcl.2010.06.136. Epub 2010 Jul 1.


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