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Articles (190)
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Mechanisms of signalling and biased agonism in G protein-coupled receptors

Wootten, Denise, Christopoulos, Arthur, Marti-Solano, Maria, Babu, M. Madan, Sexton, Patrick M.

Journal:

Nature Reviews Molecular Cell Biology

Année:

2018

Langue:

english

Fichier:

PDF, 6.08 MB

english, 2018

Allosteric Modulation of G Protein–Coupled Receptors

May, Lauren T., Leach, Katie, Sexton, Patrick M., Christopoulos, Arthur

Journal:

Annual Review of Pharmacology

Année:

2007

Langue:

english

Fichier:

PDF, 643 KB

english, 2007

Synthesis and cannabinoid activity of 1-substituted-indole-3-oxadiazole derivatives: Novel agonists for the CB1 receptor

Gerard P. Moloney, James A. Angus, Alan D. Robertson, Martin J. Stoermer, Michael Robinson, Christine E. Wright, Ken McRae, Arthur Christopoulos

Journal:

European Journal of Medicinal Chemistry

Année:

2008

Langue:

english

Fichier:

PDF, 1.44 MB

english, 2008

The Best of Both Worlds? Bitopic Orthosteric/Allosteric Ligands of G Protein–Coupled Receptors

Valant, Celine, Robert Lane, J., Sexton, Patrick M., Christopoulos, Arthur

Journal:

Annual Review of Pharmacology

Année:

2012

Langue:

english

Fichier:

PDF, 1.15 MB

english, 2012

[Handbook of Experimental Pharmacology] Muscarinic Receptors Volume 208 ||

Fryer, Allison D., Christopoulos, Arthur, Nathanson, Neil M.

Année:

2012

Langue:

english

Fichier:

PDF, 6.00 MB

english, 2012

Scheme, based on travelling-waves, for the protection of major transmission lines

Christopoulos, Christos, Thomas, D.W.P., Wright, Arthur

Journal:

IEE Proceedings C Generation Transmission and Distribution

Année:

1988

Langue:

english

Fichier:

PDF, 974 KB

english, 1988

Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders

Jeffrey Conn, P., Christopoulos, Arthur, Lindsley, Craig W.

Journal:

Nature Reviews Drug Discovery

Année:

2009

Langue:

english

Fichier:

PDF, 553 KB

english, 2009

ALLOSTERIC BINDING SITES ON CELL-SURFACE RECEPTORS: NOVEL TARGETS FOR DRUG DISCOVERY

Christopoulos, Arthur

Journal:

Nature Reviews Drug Discovery

Année:

2002

Langue:

english

Fichier:

PDF, 2.00 MB

english, 2002

A Simple Method for Quantifying Functional Selectivity and Agonist Bias

Kenakin, Terry, Watson, Christian, Muniz-Medina, Vanessa, Christopoulos, Arthur, Novick, Steven

Journal:

ACS Chemical Neuroscience

Année:

2012

Langue:

english

Fichier:

PDF, 3.92 MB

english, 2012

Allosteric modulation of G protein-coupled receptors: A pharmacological perspective

Peter Keov, Patrick M. Sexton, Arthur Christopoulos

Journal:

Neuropharmacology

Année:

2011

Langue:

english

Fichier:

PDF, 1.00 MB

english, 2011

Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology

Katie Leach, Patrick M. Sexton, Arthur Christopoulos

Journal:

Trends in Pharmacological Sciences

Année:

2007

Langue:

english

Fichier:

PDF, 660 KB

english, 2007

Signalling bias in new drug discovery: detection, quantification and therapeutic impact

Kenakin, Terry, Christopoulos, Arthur

Journal:

Nature Reviews Drug Discovery

Année:

2012

Langue:

english

Fichier:

PDF, 1.02 MB

english, 2012

Emerging paradigms in GPCR allostery: implications for drug discovery

Wootten, Denise, Christopoulos, Arthur, Sexton, Patrick M.

Journal:

Nature Reviews Drug Discovery

Année:

2013

Langue:

english

Fichier:

PDF, 1.14 MB

english, 2013

Towards tissue-specific pharmacology: insights from the calcium-sensing receptor as a paradigm for GPCR (patho)physiological bias

Leach, Katie, Conigrave, Arthur D., Sexton, Patrick M., Christopoulos, Arthur

Journal:

Trends in Pharmacological Sciences

Année:

2015

Langue:

english

Fichier:

PDF, 1.41 MB

english, 2015

Allosteric Modulation as a Unifying Mechanism for Receptor Function and Regulation

Changeux, Jean-Pierre, Christopoulos, Arthur

Journal:

Cell

Année:

2016

Langue:

english

Fichier:

PDF, 2.77 MB

english, 2016

Structure of the Adenosine A1 Receptor Reveals the Basis for Subtype Selectivity

Glukhova, Alisa, Thal, David M., Nguyen, Anh T., Vecchio, Elizabeth A., Jörg, Manuela, Scammells, Peter J., May, Lauren T., Sexton, Patrick M., Christopoulos, Arthur

Journal:

Cell

Année:

2017

Langue:

english

Fichier:

PDF, 7.46 MB

english, 2017

THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: G protein-coupled receptors

Alexander, Stephen PH, Christopoulos, Arthur, Davenport, Anthony P, Kelly, Eamonn, Marrion, Neil V, Peters, John A, Faccenda, Elena, Harding, Simon D, Pawson, Adam J, Sharman, Joanna L, Southan, Chris

Journal:

British Journal of Pharmacology

Année:

2017

Langue:

english

Fichier:

PDF, 3.71 MB

english, 2017

To Bind or Not to Bind: Unravelling GPCR Polypharmacology

Sexton, Patrick M., Christopoulos, Arthur

Journal:

Cell

Année:

2018

Langue:

english

Fichier:

PDF, 473 KB

english, 2018

Muscarinic M5 receptors modulate ethanol seeking in rats

Berizzi, Alice E., Perry, Christina J., Shackleford, David M., Lindsley, Craig W., Jones, Carrie K., Chen, Nicola A., Sexton, Patrick M., Christopoulos, Arthur, Langmead, Christopher J., Lawrence, And

Journal:

Neuropsychopharmacology

Année:

2018

Langue:

english

Fichier:

PDF, 1.31 MB

english, 2018

Extracellular loops 2 and 3 of the calcitonin receptor selectively modify agonist binding and efficacy

Dal Maso, Emma, Zhu, Yue, Pham, Vi, Reynolds, Christopher A., Deganutti, Giuseppe, Hick, Caroline A., Yang, Dehua, Christopoulos, Arthur, Hay, Debbie L., Wang, Ming-Wei, Sexton, Patrick M., Furness, S

Journal:

Biochemical Pharmacology

Année:

2018

Langue:

english

Fichier:

PDF, 5.59 MB

english, 2018

Overview of Receptor Allosterism

Christopoulos, Arthur

Journal:

Current Protocols in Pharmacology

Année:

2000

Langue:

english

Fichier:

PDF, 458 KB

english, 2000

Structural insights into G-protein-coupled receptor allostery

Thal, David M., Glukhova, Alisa, Sexton, Patrick M., Christopoulos, Arthur

Journal:

Nature

Année:

2018

Langue:

english

Fichier:

PDF, 3.25 MB

english, 2018

Kinetic and system bias as drivers of metabotropic glutamate receptor 5 allosteric modulator pharmacology

Sengmany, Kathy, Hellyer, Shane D., Albold, Sabine, Wang, Taide, Conn, P. Jeffrey, May, Lauren T., Christopoulos, Arthur, Leach, Katie, Gregory, Karen J.

Journal:

Neuropharmacology

Année:

2019

Langue:

english

Fichier:

PDF, 2.23 MB

english, 2019

3- and 6-Substituted 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridines as A1 adenosine receptor allosteric modulators and antagonists

Luigi Aurelio, Celine Valant, Heidi Figler, Bernard L. Flynn, Joel Linden, Patrick M. Sexton, Arthur Christopoulos, Peter J. Scammells

Journal:

Bioorganic & Medicinal Chemistry

Année:

2009

Langue:

english

Fichier:

PDF, 470 KB

english, 2009

Benzodiazepine ligands can act as allosteric modulators of the Type 1 cholecystokinin receptor

Fan Gao, Patrick M. Sexton, Arthur Christopoulos, Laurence J. Miller

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2008

Langue:

english

Fichier:

PDF, 455 KB

english, 2008

The synthesis and biological evaluation of 2-amino-4,5,6,7,8,9-hexahydrocycloocta[b]thiophenes as allosteric modulators of the A1 adenosine receptor

Luigi Aurelio, Arthur Christopoulos, Bernard L. Flynn, Peter J. Scammells, Patrick M. Sexton, Celine Valant

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2011

Langue:

english

Fichier:

PDF, 452 KB

english, 2011

Modulation of cannabinoid agonist binding by 5-HT in the rat cerebellum

Mark G. Devlin, Arthur Christopoulos

Journal:

Journal of Neurochemistry

Année:

2002

Langue:

english

Fichier:

PDF, 145 KB

english, 2002

Annual Scientific Meeting of ASCEPT, 1999 From ‘Captive’ Agonism To Insurmountable Antagonism: Demonstrating The Power Of Analytical Pharmacology

Arthur Christopoulos

Journal:

Clinical and Experimental Pharmacology and Physiology

Année:

2001

Langue:

english

Fichier:

PDF, 198 KB

english, 2001

ALLOSTERIC INTERACTIONS AT MUSCARINIC CHOLINOCEPTORS

Arthur Christopoulos, Alfred Lanzafame, Fred Mitchelson

Journal:

Clinical and Experimental Pharmacology and Physiology

Année:

1998

Langue:

english

Fichier:

PDF, 300 KB

english, 1998

Characterization of serotonin 5-HT2C receptor signaling to extracellular signal-regulated kinases 1 and 2

Tim D. Werry, Karen J. Gregory, Patrick M. Sexton, Arthur Christopoulos

Journal:

Journal of Neurochemistry

Année:

2005

Langue:

english

Fichier:

PDF, 801 KB

english, 2005

Pharmacological analysis of cannabinoid receptor activity in the rat vas deferens

Arthur Christopoulos, Peter Coles, Lucy Lay, Michael J Lew, James A Angus

Journal:

British Journal of Pharmacology

Année:

2001

Langue:

english

Fichier:

PDF, 215 KB

english, 2001

Effects of urea pretreatment on the binding properties of adenosine A1 receptors

Lauren T May, Patrick M Sexton, Arthur Christopoulos

Journal:

British Journal of Pharmacology

Année:

2005

Langue:

english

Fichier:

PDF, 217 KB

english, 2005

Complexing Receptor Pharmacology : Modulation of Family B G Protein–Coupled Receptor Function by RAMPs

PATRICK M. SEXTON, MARIA MORFIS, NANDA TILAKARATNE, DEBBIE L. HAY, MADHARA UDAWELA, GEORGE CHRISTOPOULOS, ARTHUR CHRISTOPOULOS

Journal:

Annals of the New York Academy of Sciences

Année:

2006

Langue:

english

Fichier:

PDF, 192 KB

english, 2006

[Handbook of Experimental Pharmacology] Muscarinic Receptors Volume 208 || Muscarinic Receptor Agonists and Antagonists: Effects on Inflammation and Immunity

Fryer, Allison D., Christopoulos, Arthur, Nathanson, Neil M.

Année:

2012

Langue:

english

Fichier:

PDF, 191 KB

english, 2012

[Handbook of Experimental Pharmacology] Muscarinic Receptors Volume 208 || Overview of Muscarinic Receptor Subtypes

Fryer, Allison D., Christopoulos, Arthur, Nathanson, Neil M.

Année:

2012

Langue:

english

Fichier:

PDF, 223 KB

english, 2012

[Handbook of Experimental Pharmacology] Muscarinic Receptors Volume 208 || Muscarinic Receptors in Brain Stem and Mesopontine Cholinergic Arousal Functions

Fryer, Allison D., Christopoulos, Arthur, Nathanson, Neil M.

Année:

2012

Langue:

english

Fichier:

PDF, 317 KB

english, 2012

[Handbook of Experimental Pharmacology] Muscarinic Receptors Volume 208 || Muscarinic Receptor Agonists and Antagonists: Effects on Cardiovascular Function

Fryer, Allison D., Christopoulos, Arthur, Nathanson, Neil M.

Année:

2012

Langue:

english

Fichier:

PDF, 270 KB

english, 2012

[Handbook of Experimental Pharmacology] Muscarinic Receptors Volume 208 || Muscarinic Receptor Agonists and Antagonists: Effects on Ocular Function

Fryer, Allison D., Christopoulos, Arthur, Nathanson, Neil M.

Année:

2012

Langue:

english

Fichier:

PDF, 293 KB

english, 2012

[Handbook of Experimental Pharmacology] Muscarinic Receptors Volume 208 || Activation of Muscarinic Receptors by Non-neuronal Acetylcholine

Fryer, Allison D., Christopoulos, Arthur, Nathanson, Neil M.

Année:

2012

Langue:

english

Fichier:

PDF, 457 KB

english, 2012

Binding of the muscarine receptor antagonist heptane-1,7-bis(dimethyl-3′-phthalimidopropyl) ammonium bromide at cholinoceptor sites: European Journal of Pharmacology - Molecular Pharmacology Section, 246 (1993) 1–8

Arthur Christopoulos, Richard Loiacono, Fred Mitchelson

Journal:

European Journal of Pharmacology: Molecular Pharmacology

Année:

1993

Langue:

english

Fichier:

PDF, 48 KB

english, 1993

Binding of the muscarine receptor antagonist heptane-1,7-bis(dimethyl-3′-phthalimidopropyl) ammonium bromide at cholinoceptor sites

Arthur Christopoulos, Richard Loiacono, Fred Mitchelson

Journal:

European Journal of Pharmacology: Molecular Pharmacology

Année:

1993

Langue:

english

Fichier:

PDF, 743 KB

english, 1993

[3H]N-methylscopolamine dissociation from muscarine receptors affected by low concentrations of allosteric modulators

Arthur Christopoulos, Fred Mitchelson

Journal:

European Journal of Pharmacology: Molecular Pharmacology

Année:

1995

Langue:

english

Fichier:

PDF, 301 KB

english, 1995

Effects of anandamide on the binding and signaling properties of M1 muscarinic acetylcholine receptors

Alfred A. Lanzafame, Elizabeth Guida, Arthur Christopoulos

Journal:

Biochemical Pharmacology

Année:

2004

Langue:

english

Fichier:

PDF, 273 KB

english, 2004

Pharmacology of 5HT2C receptor-mediated ERK1/2 phosphorylation: Agonist-specific activation pathways and the impact of RNA editing

Tim D. Werry, Gregory D. Stewart, Michael F. Crouch, Anne Watts, Patrick M. Sexton, Arthur Christopoulos

Journal:

Biochemical Pharmacology

Année:

2008

Langue:

english

Fichier:

PDF, 442 KB

english, 2008

Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6-tetrahydropyridines as 5-HT2C agonists

Richard J. Conway, Celine Valant, Arthur Christopoulos, Alan D. Robertson, Ben Capuano, Ian T. Crosby

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2012

Langue:

english

Fichier:

PDF, 1.25 MB

english, 2012

The effect of social isolation on rat brain expression of genes associated with endocannabinoid signaling

Stephanie A. Robinson, Richard E. Loiacono, Arthur Christopoulos, Patrick M. Sexton, Daniel T. Malone

Journal:

Brain Research

Année:

2010

Langue:

english

Fichier:

PDF, 1.12 MB

english, 2010

Modulating receptor function through RAMPs: can they represent drug targets in themselves?

Patrick M. Sexton, David R. Poyner, John Simms, Arthur Christopoulos, Debbie L. Hay

Journal:

Drug Discovery Today

Année:

2009

Langue:

english

Fichier:

PDF, 590 KB

english, 2009

Regulation of serotonin 5-HT2C receptors by chronic ligand exposure

Mark G. Devlin, Nicola J. Smith, Olivia M. Ryan, Elizabeth Guida, Patrick M. Sexton, Arthur Christopoulos

Journal:

European Journal of Pharmacology

Année:

2004

Langue:

english

Fichier:

PDF, 305 KB

english, 2004

RNA editing of the serotonin 5HT2C receptor and its effects on cell signalling, pharmacology and brain function

Tim D. Werry, Richard Loiacono, Patrick M. Sexton, Arthur Christopoulos

Journal:

Pharmacology & Therapeutics

Année:

2008

Langue:

english

Fichier:

PDF, 1.26 MB

english, 2008

Allostery in GPCRs: ‘MWC’ revisited

Meritxell Canals, Patrick M. Sexton, Arthur Christopoulos

Journal:

Trends in Biochemical Sciences

Année:

2011

Langue:

english

Fichier:

PDF, 1.09 MB

english, 2011