Charlton, Steven - University of Nottingham

个人简介

Prof Charlton joined the University of Nottingham in 2014 where he is Professor of Molecular Pharmacology and Drug Discovery in the School of Life Sciences. Prior to that he spent 16 years in the pharmaceutical industry, both at SmithKline Beecham and Novartis. At Novartis he was Director of Molecular Pharmacology in Respiratory Diseases, leading an assay development and compound profiling team of over 30 scientists providing expert opinion and support for GPCR, ion channel and enzyme projects. He has broad drug discovery experience, ranging from target validation through to leading full lead optimisation programmes to successful clinical proof of concept. He also served on global development teams for several inhaled compounds in Ph2, Ph3 and post-launch, including Onbrez™, Seebri™ and UltiBro™. In 2007 Prof Charlton was awarded Novartis Leading Scientist in recognition of his contribution to the field of quantitative pharmacology and to the Novartis pipeline.

近期论文

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BERGSDORF, CHRISTIAN, FIEZ-VANDAL, CEDRIC, SYKES, DAVID A., BERNET, PASCAL, AUSSENAC, SONIA, CHARLTON, STEVEN J., SCHOPFER, ULRICH, OTTL, JOHANNES and DUCKELY, MYRIAM, 2016. An Alternative Thiol-Reactive Dye to Analyze Ligand Interactions with the Chemokine Receptor CXCR2 Using a New Thermal Shift Assay Format JOURNAL OF BIOMOLECULAR SCREENING. 21(3), 243-251 ROSETHORNE EM, BRADLEY ME, GHERBI K, SYKES DA, SATTIKAR A, WRIGHT JD, RENARD E, TRIFILIEFF A, FAIRHURST RA and CHARLTON SJ, 2016. Long Receptor Residence Time of C26 Contributes to Super Agonist Activity at the Human β2 Adrenoceptor. Molecular pharmacology. 89(4), 467-75 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 and LANE JR, 2016. The role of kinetic context in apparent biased agonism at GPCRs. Nature communications. 7, 10842 SYKES DA, BRADLEY ME, RIDDY DM, WILLARD E, REILLY J, MIAH A, BAUER C, WATSON SJ, SANDHAM DA, DUBOIS G and CHARLTON SJ, 2016. Fevipiprant (QAW039), a Slowly Dissociating CRTh2 Antagonist with the Potential for Improved Clinical Efficacy. Molecular pharmacology. 89(5), 593-605 DICKSON CJ, HORNAK V, VELEZ-VEGA C, MCKAY DJ, REILLY J, SANDHAM DA, SHAW D, FAIRHURST RA, CHARLTON SJ, SYKES DA, PEARLSTEIN RA and DUCA JS, 2016. Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding. Journal of medicinal chemistry. 59(12), 5780-9 BRADLEY, M. E., DOMBRECHT, B., MANINI, J., WILLIS, J., VLERICK, D., DE TAEYE, S., VAN DEN HEEDE, K., ROOBROUCK, A., GROT, E., KENT, T. C., LAEREMANS, T., STEFFENSEN, S., VAN HEEKE, G., BROWN, Z., CHARLTON, S. J. and CROMIE, K. D., 2015. Potent and Efficacious Inhibition of CXCR2 Signaling by Biparatopic Nanobodies Combining Two Distinct Modes of Action MOLECULAR PHARMACOLOGY. 87(2), 251-262 VAUQUELIN, GEORGES, HALL, DAVID and CHARLTON, STEVEN J., 2015. 'Partial' competition of heterobivalent ligand binding may be mistaken for allosteric interactions: a comparison of different target interaction models BRITISH JOURNAL OF PHARMACOLOGY. 172(9), 2300-2315 ROSETHORNE EM, BRADLEY ME, KENT TC and CHARLTON SJ, 2015. Functional desensitization of the β 2 adrenoceptor is not dependent on agonist efficacy. Pharmacology research & perspectives. 3(1), e00101 TRIFILIEFF A, ETHELL BT, SYKES DA, WATSON KJ, COLLINGWOOD S, CHARLTON SJ and KENT TC, 2015. Comparing the cardiovascular therapeutic indices of glycopyrronium and tiotropium in an integrated rat pharmacokinetic, pharmacodynamic and safety model. Toxicology and applied pharmacology. 287(1), 9-16 BLAKELEY D, SYKES DA, ENSOR P, BERTRAN E, ASTON PJ and CHARLTON SJ, 2015. 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. British journal of pharmacology. 172(21), 5037-49 BERGSDORF C, FIEZ-VANDAL C, SYKES DA, BERNET P, AUSSENAC S, CHARLTON SJ, SCHOPFER U, OTTL J and DUCKELY M, 2015. An Alternative Thiol-Reactive Dye to Analyze Ligand Interactions with the Chemokine Receptor CXCR2 Using a New Thermal Shift Assay Format. Journal of biomolecular screening. 21(3), 243-51 DALE, PHILIPPA R., CERNECKA, HANA, SCHMIDT, MARTINA, DOWLING, MARK R., CHARLTON, STEVEN J., PIEPER, MICHAEL P. and MICHEL, MARTIN C., 2014. The pharmacological rationale for combining muscarinic receptor antagonists and beta-adrenoceptor agonists in the treatment of airway and bladder disease CURRENT OPINION IN PHARMACOLOGY. 16, 31-42 MACKENZIE, AMANDA E., CALTABIANO, GIANLUIGI, KENT, TOBY C., JENKINS, LAURA, MCCALLUM, JENNIFER E., HUDSON, BRIAN D., NICKLIN, STUART A., FAWCETT, LINDSAY, MARKWICK, RACHEL, CHARLTON, STEVEN J. and MILLIGAN, GRAEME, 2014. The Antiallergic Mast Cell Stabilizers Lodoxamide and Bufrolin as the First High and Equipotent Agonists of Human and Rat GPR35 MOLECULAR PHARMACOLOGY. 85(1), 91-104 SANDHAM, DAVID A., CHARLTON, STEVEN J., DUBOIS, GERALD, ERPENBECK, VEIT J., SYKES, DAVID and WATSON, SIMON J., 2014. Discovery and characterisation of CRTh2 receptor antagonists suitable for clinical testing in allergic diseases ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY. 248, BILL, ANKE, ROSETHORNE, ELIZABETH M., KENT, TOBY C., FAWCETT, LINDSAY, BURCHELL, LYNN, VAN DIEPEN, MICHIEL T., MARELLI, ANTHONY, BATALOV, SERGEY, MIRAGLIA, LOREN, ORTH, ANTHONY P., RENAUD, NICOLE A., CHARLTON, STEVEN J., GOSLING, MARTIN, GAITHER, L. ALEX and GROOT-KORMELINK, PAUL J., 2014. High Throughput Mutagenesis for Identification of Residues Regulating Human Prostacyclin (hIP) Receptor Expression and Function PLOS ONE. 9(6), MCKEOWN, STEPHEN C., CHARLTON, STEVEN J., COX, BRIAN, FITCH, HELEN, HOWSON, CHRISTOPHER D., LEBLANC, CATHERINE, MEYER, ARNDT, ROSETHORNE, ELIZABETH M. and STANLEY, EMILY, 2014. Identification of novel IP receptor agonists using historical ligand biased chemical arrays BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. 24(10), 2247-2250 SYKES, DAVID A., PARRY, CHERYL, REILLY, JOHN, WRIGHT, PENNY, FAIRHURST, ROBIN A. and CHARLTON, STEVEN J., 2014. Observed Drug-Receptor Association Rates Are Governed by Membrane Affinity: The Importance of Establishing "Micro-Pharmacokinetic/Pharmacodynamic Relationships" at the beta(2)-Adrenoceptor MOLECULAR PHARMACOLOGY. 85(4), 608-617 SYKES, DAVID A., RIDDY, DARREN M., STAMP, CRAIG, BRADLEY, MICHELLE E., MCGUINESS, NEIL, SATTIKAR, AFRAH, GUERINI, DANILO, RODRIGUES, INES, GLAENZEL, ALBRECHT, DOWLING, MARK R., MULLERSHAUSEN, FLORIAN and CHARLTON, STEVEN J., 2014. Investigating the molecular mechanisms through which FTY720-P causes persistent S1P(1) receptor internalization BRITISH JOURNAL OF PHARMACOLOGY. 171(21), 4797-4807 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 and TUFFNELL A, 2014. The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting β2-adrenoceptor agonist. Bioorganic & medicinal chemistry letters. 24(17), 4341-7 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 and PRESS NJ, 2014. The discovery of potent, orally bioavailable pyrimidine-5-carbonitrile-6-alkyl CXCR2 receptor antagonists. Bioorganic & medicinal chemistry letters. 24(15), 3285-90 ROSETHORNE, ELIZABETH M, KENT, TOBY C, FAWCETT, LINDSAY, VAN DIEPEN, MICHIEL T, MARELLI, ANTHONY, BATALOV, SERGEY, CHARLTON, STEVEN J, GOSLING, MARTIN, GAITHER, L ALEX, RENAUD, NICOLE A, GROOT-KORMELINK, PAUL J, ORTH, ANTHONY P, BURCHELL, LYNN, MIRAGLIA, LOREN and BILL, ANKE, 2014. Colony number and mutation rate obtained by hydroxyl amine mediated mutagenesis. Figshare. 1, 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 and CROMIE KD, 2014. Potent and efficacious inhibition of CXCR2 signaling by biparatopic nanobodies combining two distinct modes of action. Molecular pharmacology. 87(2), 251-62 VAUQUELIN G, HALL D and CHARLTON SJ, 2014. 'Partial' competition of heterobivalent ligand binding may be mistaken for allosteric interactions: a comparison of different target interaction models. British journal of pharmacology. 172(9), 2300-15 NIJMEIJER, S., VISCHER, H. F., SIRCI, F., SCHULTES, S., ENGELHARDT, H., DE GRAAF, C., ROSETHORNE, E. M., CHARLTON, S. J. and LEURS, R., 2013. Detailed analysis of biased histamine H-4 receptor signalling by JNJ 7777120 analogues BRITISH JOURNAL OF PHARMACOLOGY. 170(1), 78-88 RIAZ, SAJJAD A., CHARLTON, STEVEN J. and TOBIN, ANDREW B., 2013. STUDIES TO VALIDATE A CHEMICAL GENETIC APPROACH TO INVESTIGATE THE M1 MUSCARINIC RECEPTOR JOURNAL OF RECEPTORS AND SIGNAL TRANSDUCTION. 33(3), 201-201