Mandarin Translations


To cite any of the articles below, please refer to the full article and not the DOI of this translations section. inline image

Themed section: molecular pharmacology of GPCRs inline image

RJ Summers1,2

1Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Vic, Australia, and2Department of Pharmacology, Monash University, Clayton, Vic, Australia

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To view the full version of this article please visit http://dx.doi.org/10.1111/j.1476-5381.2011.01679.xinline imagehttp://dx.doi.org/10.1111/j.1476-5381.2011.01679.x

GPCR expression in tissues and cells: Are the optimal receptors being used as drug targets? inline image

PA Insel1,2, A Snead1, F Murray2, L Zhang1, H Yokouchi1, T Katakia1, O Kwon1, D Dimucci1 and A Wilderman1

1Departments of Pharmacology and 2Medicine, University of California, San Diego, La Jolla, CA, USA

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To view the full version of this article please visit http://dx.doi.org/10.1111/j.1476-5381.2011.01434.xinline imagehttp://dx.doi.org/10.1111/j.1476-5381.2011.01434.x

Pharmacological modulation of chemokine receptor function inline image

DJ Scholten, M Canals, D Maussang, L Roumen, MJ Smit, M Wijtmans, C de Graaf, HF Vischer and R Leurs

Leiden/Amsterdam Center for Drug Research, Division of Medicinal Chemistry, Faculty of Science, VU University Amsterdam, Amsterdam, The Netherlands

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To view the full version of this article please visit http://dx.doi.org/10.1111/j.1476-5381.2011.01551.xinline imagehttp://dx.doi.org/10.1111/j.1476-5381.2011.01551.x

Constitutive formation of an RXFP1–signalosome: a novel paradigm in GPCR function and regulation inline image

Michelle L Halls

Department of Pharmacology, University of Cambridge, Cambridge, UK

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To view the full version of this article please visit http://dx.doi.org/10.1111/j.1476-5381.2011.01470.xinline imagehttp://dx.doi.org/10.1111/j.1476-5381.2011.01470.x

Biased signalling and allosteric machines: new vistas and challenges for drug discovery inline image

Terry P Kenakin

Department of Pharmacology, University of North Carolina, Chapel Hill, North Carolina, USA

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To view the full version of this article please visit http://dx.doi.org/10.1111/j.1476-5381.2011.01749.xinline imagehttp://dx.doi.org/10.1111/j.1476-5381.2011.01749.x

Behind the curtain: cellular mechanisms for allosteric modulation of calcium-sensing receptors inline image

Alice Cavanaugh1, Ying Huang2 and Gerda E Breitwieser1

1Weis Center for Research, Geisinger Clinic, Danville, PA, USA, and2Cancer Drug Research Laboratory, McGill University/Royal Victoria Hospital, Montreal, QC, Canada

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To view the full version of this article please visit http://dx.doi.org/10.1111/j.1476-5381.2011.01403.xinline imagehttp://dx.doi.org/10.1111/j.1476-5381.2011.01403.x

The orexin receptor OX1R in colon cancer: a promising therapeutic target and a new paradigm in G protein-coupled receptor signalling through ITIMs inline image

Marc Laburthe1,2 and Thierry Voisin1,2

1INSERM, U773, Centre de Recherche Biomédicale Bichat Beaujon CRB3, Paris, France, and2Université Paris Diderot, Paris, France

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To view the full version of this article please visit http://dx.doi.org/10.1111/j.1476-5381.2011.01510.xinline imagehttp://dx.doi.org/10.1111/j.1476-5381.2011.01510.x

Lifting the lid on GPCRs: the role of extracellular loops inline image

M Wheatley1, D Wootten2,3, MT Conner4, J Simms2,3, R Kendrick1, RT Logan1, DR Poyner4 and J Barwell4

1School of Biosciences, University of Birmingham, Birmingham, UK,2Drug Discovery Biology Laboratory, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia,3Department of Pharmacology, Monash University, Parkville, Victoria, Australia, and4School of Life and Health Sciences, Aston University, Aston Triangle, Birmingham, UK

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To view the full version of this article please visit http://dx.doi.org/10.1111/j.1476-5381.2011.01629.xinline imagehttp://dx.doi.org/10.1111/j.1476-5381.2011.01629.x

Mechanisms of rapid opioid receptor desensitization, resensitization and tolerance in brain neurons inline image

Vu C Dang1 and MacDonald J Christie2

1Department of Psychiatry, University of California, San Francisco, CA, USA and2Brain & Mind Research Institute, University of Sydney, NSW, Australia

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Regulation of GPCR activity, trafficking and localization by GPCR-interacting proteins inline image

Ana C Magalhaes1,2, Henry Dunn1,2 and Stephen SG Ferguson1,2

1J.Allyn Taylor Centre for Cell Biology, Molecular Brain Research Group, Robarts Research Institute, London, ON, Canada, and2The Department of Physiology & Pharmacology, the University of Western Ontario, London, ON, Canada

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To view the full version of this article please visit http://dx.doi.org/10.1111/j.1476-5381.2011.01552.xinline imagehttp://dx.doi.org/10.1111/j.1476-5381.2011.01552.x

Corticosteroid-induced gene expression in allergen-challenged asthmatic subjects taking inhaled budesonide inline image

MM Kelly1, EM King1, CF Rider1, C Gwozd1, NS Holden1, J Eddleston2, B Zuraw2, R Leigh1, PM O'Byrne3 and R Newton1

1Airways Inflammation Research Group, Institute of Infection, Immunity and Inflammation, Faculty of Medicine, University of Calgary, Calgary, AB, Canada,2Allergy and Immunology Section, University of California, San Diego School of Medicine, La Jolla, CA, USA, and3Firestone Institute for Respiratory Health, St.Joseph's Hospital and the Department of Medicine, McMaster University, Hamilton, ON, Canada

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To view the full version of this article please visit http://dx.doi.org/10.1111/j.1476-5381.2011.01620.xinline imagehttp://dx.doi.org/10.1111/j.1476-5381.2011.01620.x

Ketamine-induced ventricular structural, sympathetic and electrophysiological remodelling: pathological consequences and protective effects of metoprolol inline image

Y Li1, J Shi1, BF Yang2, L Liu1, CL Han1, WM Li1, DL Dong2, ZW Pan2, GZ Liu1, JQ Geng1, L Sheng1, XY Tan1, DH Sun1, ZH Gong1 and YT Gong1

1Cardiovascular Department, the First Clinical Hospital and2Department of Pharmacology and Bio-pharmaceutical Key Laboratory of Heilongjiang Province and State, Harbin Medical University, Harbin, China

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To view the full version of this article please visit http://dx.doi.org/10.1111/j.1476-5381.2011.01635.xinline imagehttp://dx.doi.org/10.1111/j.1476-5381.2011.01635.x

Different in vitro and in vivo profiles of substituted 3-aminopropylphosphinate and 3-aminopropyl(methyl) phosphinate GABAB receptor agonists as inhibitors of transient lower oesophageal sphincter relaxation inline image

A Lehmann1, M Antonsson1, A Aurell-Holmberg1, LA Blackshaw2, L Brändén1, T Elebring1, J Jensen1, L Kärrberg1, JP Mattsson1, K Nilsson1, SS Oja3, P Saransaari4 and S von Unge1

1AstraZeneca R&D, Mölndal, Sweden, and2Nerve Gut Research Laboratory, Hanson Institute, Department of Gastroenterology and Hepatology, Royal Adelaide Hospital, and University of Adelaide, South Australia, Australia, and3Department of Paediatrics, Tampere University Hospital, Finland, and4Brain Research Center, Medical School, University of Tampere, Finland

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To view the full version of this article please visit http://dx.doi.org/10.1111/j.1476-5381.2011.01682.xinline imagehttp://dx.doi.org/10.1111/j.1476-5381.2011.01682.x

Cannabinoid CB2 receptors modulate ERK-1/2 kinase signalling and NO release in microglial cells stimulated with bacterial lipopolysaccharide inline image

Stefania Merighi1, Stefania Gessi1, Katia Varani1, Carolina Simioni1, Debora Fazzi1, Prisco Mirandola2 and Pier Andrea Borea1

1Department of Clinical and Experimental Medicine, Pharmacology Section and Interdisciplinary Center for the Study of Inflammation, University of Ferrara, Via Fossato di Mortara, Ferrara, Italy, and2Department of Human Anatomy, Pharmacology and Forensic Medicine, Institute of Normal Human Anatomy, Ospedale Maggiore, University of Parma, Parma, Italy

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To view the full version of this article please visit http://dx.doi.org/10.1111/j.1476-5381.2011.01673.xinline imagehttp://dx.doi.org/10.1111/j.1476-5381.2011.01673.x

A novel fluorescent histamine H1 receptor antagonist demonstrates the advantage of using fluorescence correlation spectroscopy to study the binding of lipophilic ligands inline image

Rachel H Rose, Stephen J Briddon and Stephen J Hill

Institute of Cell Signalling, School of Biomedical Sciences, University of Nottingham, Nottingham, UK

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To view the full version of this article please visit http://dx.doi.org/10.1111/j.1476-5381.2011.01640.xinline imagehttp://dx.doi.org/10.1111/j.1476-5381.2011.01640.x

Structure-activity relationships of vanilloid receptor agonists for arteriolar TRPV1 inline image

Á Czikora1, E Lizanecz1, P Bakó1, I Rutkai1, F Ruzsnavszky2, J Magyar2, R Pórszász3, T Kark3, A Facskó4, Z Papp1,5, I Édes1,5 and A Tóth1,5

1Division of Clinical Physiology, Institute of Cardiology;2Department of Physiology,3Department of Pharmacology and Pharmacotherapy, Institute of Pharmacology,4Department of Ophthalmology, and5Research Centre for Molecular Medicine, Medical and Health Science Center, University of Debrecen, Debrecen, Hungary

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To view the full version of this article please visit http://dx.doi.org/10.1111/j.1476-5381.2011.01645.xinline imagehttp://dx.doi.org/10.1111/j.1476-5381.2011.01645.x

Ursolic acid induces apoptosis in human leukaemia cells and exhibits anti-leukaemic activity in nude mice through the PKB pathway inline image

Ning Gao1,2, Senping Cheng2, Amit Budhraja2, Ziyi Gao2, Jieping Chen3, E-Hu Liu1, Cheng Huang2, Deying Chen1, Zailin Yang3, Qun Liu4, Ping Li4, Xianglin Shi2 and Zhuo Zhang2

1Department of Pharmacognosy, College of Pharmacy, 3rd Military Medical University, Chongqing, China;2Graduate Center for Toxicology, College of Medicine, University of Kentucky, Lexington, Kentucky;3Department of Hematology, Southwest Hospital, 3rd Military Medical University, Chongqing, China;4Key Laboratory of Modern Chinese Medicines (China Pharmaceutical University), Ministry of Education, Nanjing, China

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To view the full version of this article please visit http://dx.doi.org/10.1111/j.1476-5381.2011.01684.xinline imagehttp://dx.doi.org/10.1111/j.1476-5381.2011.01684.x

Antiplatelet and antithrombotic effect of F 16618, a new thrombin proteinase-activated receptor-1 (PAR1) antagonist inline image

M Dumas1,2, F Nadal-Wollbold3, P Gaussem1,2,4, M Perez3, T Mirault1,2,4, R Létienne3, T Bourbon3, F Grelac1,2, B Le Grand3 and C Bachelot-Loza1,2

1Inserm UMR S 765, Faculté de Pharmacie, Paris, France,2Université Paris Descartes, Sorbonne Paris Cité, Paris, France,3Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin, Castres cedex, France, and4AP-HP, Hôpital Européen Georges Pompidou, Service d'Hématologie Biologique, Paris, France

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Identification of drugs and drug metabolites as substrates of multidrug resistance protein 2 (MRP2) using triple-transfected MDCK-OATP1B1-UGT1A1-MRP2 cells inline image

C Fahrmayr, J König, D Auge, M Mieth and MF Fromm

Institute of Experimental and Clinical Pharmacology and Toxicology, Friedrich-Alexander-Universität Erlangen-Nürnberg, Erlangen, Germany

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To view the full version of this article please visit http://dx.doi.org/10.1111/j.1476-5381.2011.01672.xinline imagehttp://dx.doi.org/10.1111/j.1476-5381.2011.01672.x

Predicting the emetic liability of novel chemical entities: a comparative study inline image

Nathalie Percie du Sert1,2, Anthony M Holmes1, Rob Wallis3 and Paul LR Andrews2

1The National Centre for the Replacement, Refinement and Reduction of Animals in Research, London, UK,2Division of Biomedical Sciences, St George's University of London, London, UK, and3Pfizer Drug Safety Research and Development, Groton, CT, USA

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Inhibitory effect of bufalin and cinobufagin on steroidogenesis via the activation of ERK in human adrenocortical cells inline image

Mei-Mei Kau1, Jiing-Rong Wang2, Shiow-Chwen Tsai3, Ching-Han Yu4 and Paulus S Wang5

1Center of General Education, National Taipei University of Nursing and Health Sciences, Taipei, Taiwan,2Department of Pathology and Laboratory Medicine, Shin Kong Wu Ho-Su Memorial Hospital, Taipei, Taiwan,3Graduate Institute of Transition and Leisure Education for Individuals with Disabilities, Taipei Physical Education College, Taipei, Taiwan,4Department of Physiology, School of Medicine, Chung Shan Medical University, Taichung, Taiwan, and5Department of Physiology, School of Medicine, National Yang-Ming University, Taipei, Taiwan

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To view the full version of this article please visit http://dx.doi.org/10.1111/j.1476-5381.2011.01671.xinline imagehttp://dx.doi.org/10.1111/j.1476-5381.2011.01671.x

Roflumilast inhibits the release of chemokines and TNF-α from human lung macrophages stimulated with lipopolysaccharide inline image

A Buenestado1, S Grassin-Delyle1,F Guitard1, E Naline1, C Faisy1,2, D Israël-Biet3, E Sage4, JF Bellamy5, H Tenor6 and P Devillier1

1Laboratory of Pulmonary Pharmacology UPRES EA220, Foch Hospital, University Versailles Saint-Quentin, Suresnes, France,2Medical Intensive Care Unit, Georges Pompidou European Hospital, Paris, France,3Department of Pneumology University Paris-Descartes, APHP, Georges Pompidou European Hospital, Paris, France,4Department of Thoracic Surgery, Foch Hospital, University Versailles Saint-Quentin, Suresnes, France,5Thoracic Surgery, Val d'Or Clinic, Saint-Cloud, France, and6Department of Biology, Nycomed, Konstanz, Germany

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A novel angiopoietin-derived peptide displays anti-angiogenic activity and inhibits tumour-induced and retinal neovascularization inline image

GM Palmer1, Z Tiran2, Z Zhou3, ME Capozzi4, W Park1, C Coletta3, A Pyriochou3, Y Kliger2, O Levy2, I Borukhov2, MW Dewhirst1, G Rotman2, JS Penn4 and A Papapetropoulos3

1Department of Radiation Oncology, Duke University Medical Center, Durham, NC, USA,2Compugen Ltd, Tel-Aviv, Israel,3Laboratory for Molecular Pharmacology, Department of Pharmacy, University of Patras, Patras, Greece, and4Department of Ophthalmology and Visual Sciences, Vanderbilt University School of Medicine, Nashville, TN, USA

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To view the full version of this article please visit http://dx.doi.org/10.1111/j.1476-5381.2011.01677.xinline imagehttp://dx.doi.org/10.1111/j.1476-5381.2011.01677.x

Polymorphisms of ADORA2A modulate psychomotor vigilance and the effects of caffeine on neurobehavioural performance and sleep EEG after sleep deprivation inline image

S Bodenmann1, C Hohoff2, C Freitag3, J Deckert2,4, J V Rétey1, V Bachmann1,5 and H-P Landolt1,5

1Institute of Pharmacology and Toxicology, University of Zürich, Zürich, Switzerland,2Department of Psychiatry, University of Münster, Münster, Germany,3Department of Child and Adolescent Psychiatry, Psychosomatics and Psychotherapy, Johann-Wolfgang Goethe University, Frankfurt am Main, Germany,4Department of Psychiatry, University of Würzburg, Würzburg, Germany and5Zürich Center for Integrative Human Physiology, University of Zürich, Zürich, Switzerland

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Hydrogen sulphide-releasing diclofenac derivatives inhibit breast cancer-induced osteoclastogenesis in vitro and prevent osteolysis ex vivoinline image

J Frantzias1, JG Logan1,2, P Mollat3, A Sparatore4, P Del Soldato5, SH Ralston2 and AI Idris1,2

1The Centre for Molecular Medicine, Institute of Genetics and Molecular Medicine, University of Edinburgh, Western General Hospital, Edinburgh, UK,2Edinburgh Cancer Research Centre, Institute of Genetics and Molecular Medicine, University of Edinburgh, Western General Hospital, Edinburgh, UK,3Galapagos SASU, Romainville, France,4Department of Pharmaceutical Sciences ‘P.Pratesi’, Università degli Studi di Milano, Milan, Italy, and5CTG Pharma S.r.l., Milan, Italy

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To view the full version of this article please visit http://dx.doi.org/10.1111/j.1476-5381.2011.01704.xinline imagehttp://dx.doi.org/10.1111/j.1476-5381.2011.01704.x

Potent anti-inflammatory effect of a novel furan-2,5-dione derivative, BPD, mediated by dual suppression of COX-2 activity and LPS-induced inflammatory gene expression via NF-κB inactivation inline image

Ji-Sun Shin1,3, Seung-Jae Park1,3, Suran Ryu1,3, Han Byul Kang4, Tae Woo Kim4, Jung-Hye Choi2,5, Jae-Yeol Lee4, Young-Wuk Cho3 and Kyung-Tae Lee1,2,3

1Department of Pharmaceutical Biochemistry, College of Pharmacy, Kyung Hee University, Seoul, Korea,2Department of Life and Nanopharmaceutical Science, College of Pharmacy, Kyung Hee University, Seoul, Korea,3Department of Biomedical Science, College of Medical Science, Kyung Hee University, Seoul, Korea,4Research Institute for Basic Sciences and Department of Chemistry, College of Sciences, Kyung Hee University, Seoul, Korea, and5Department of Oriental Pharmaceutical Science, College of Pharmacy, Kyung Hee University, Seoul, Korea

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To view the full version of this article please visit http://dx.doi.org/10.1111/j.1476-5381.2011.01670.xinline imagehttp://dx.doi.org/10.1111/j.1476-5381.2011.01670.x

D-Amino acid oxidase-mediated increase in spinal hydrogen peroxide is mainly responsible for formalin-induced tonic pain inline image

Jin-Miao Lu, Nian Gong, Yan-Chao Wang and Yong-Xiang Wang

King's Lab, School of Pharmacy, Shanghai Jiao Tong University, Shanghai, China

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Role of 5-HT1 receptor subtypes in the modulation of pain and synaptic transmission in rat spinal superficial dorsal horn inline image

Hyo-Jin Jeong, Vanessa A Mitchell and Christopher W Vaughan

Pain Management Research Institute, Kolling Institute of Medical Research, Northern Clinical School, University of Sydney at Royal North Shore Hospital, NSW, Australia

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Modulation of mouse gastrointestinal motility by allyl isothiocyanate, a constituent of cruciferous vegetables (Brassicaceae): evidence for TRPA1-independent effects inline image

Raffaele Capasso1, Gabriella Aviello1, Barbara Romano1, Francesca Borrelli1, Luciano De Petrocellis2, Vincenzo Di Marzo2 and Angelo A Izzo1

1Department of Experimental Pharmacology, Endocannabinoid Research Group, University of Naples Federico II, Naples, Italy and2Institute of Biomolecular Chemistry, Endocannabinoid Research Group, National Research Council, Pozzuoli (NA), Italy

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TNF-α-induced airway hyperresponsiveness to cholinergic stimulation in guinea pig airways inline image

R Makwana1, N Gozzard2, D Spina1 and C Page1

1Sackler Institute of Pulmonary Pharmacology, Institute of Pharmaceutical Science, King's College London, London, UK, and2UCB Celltech, Slough, UK

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Role of endothelin-1 in the hyper-responsiveness to nitrovasodilators following acute NOS inhibition inline image

Stephane L Bourque1, Heather A Whittingham2, Susan E Brien2, Sandra T Davidge1 and Michael A Adams2

1Department of Obstetrics and Gynecology, University of Alberta, Edmonton, Alberta, Canada, and2Department of Pharmacology and Toxicology, Queen's University, Kingston, Ontario, Canada

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Comparative effects of different modes of renin angiotensin system inhibition on hypercholesterolaemia-induced atherosclerosis inline image

Hong Lu1, Anju Balakrishnan1, Deborah A Howatt1, Congqing Wu2, Richard Charnigo3, Gene Liau4, Lisa A Cassis2 and Alan Daugherty1,2

1Saha Cardiovascular Research Center,2Graduate Center for Nutritional Sciences and3Department of Statistics, University of Kentucky, Lexington, KY, USA, and4Novartis Institutes for Biomedical Research, Cambridge, MA, USA

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