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Arthur Christopoulos

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Vimesh A Avlani; Arthur Christopoulos; Leigh Delbridge; Katie Leach; Wenting Ma; Hee-Chang Mun; Arthur D Conigrave
Calcium-sensing receptor-dependent activation of CREB phosphorylation in HEK293 cells and human parathyroid cells.
Christopher J Langmead; Arthur Christopoulos
Supra-physiological efficacy at GPCRs: superstition or super agonists?
Joshua H Y Tan; Jamie Wedderburn; Deni Taleski; Stephen J Butler; Meritxell Canals; Arthur Christopoulos; Pam Hall; Michael J Hickey; Justin P Ludeman; Richard J Payne; Martin J Stone
Tyrosine sulfation of chemokine receptor CCR2 enhances interactions with both monomeric and dimeric forms of the chemokine monocyte chemoattractant protein-1 (MCP-1).

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2013: Vimesh A Avlani; Arthur Christopoulos; Leigh Delbridge; Katie Leach; Wenting Ma; Hee-Chang Mun; Arthur D Conigrave
Calcium-sensing receptor-dependent activation of CREB phosphorylation in HEK293 cells and human parathyroid cells.
American journal of physiology. Endocrinology and metabolism 2013;304(10):E1097-104.
2013: Christopher J Langmead; Arthur Christopoulos
Supra-physiological efficacy at GPCRs: superstition or super agonists?
British journal of pharmacology 2013;169(2):353-6.
2013: Joshua H Y Tan; Jamie Wedderburn; Deni Taleski; Stephen J Butler; Meritxell Canals; Arthur Christopoulos; Pam Hall; Michael J Hickey; Justin P Ludeman; Richard J Payne; Martin J Stone
Tyrosine sulfation of chemokine receptor CCR2 enhances interactions with both monomeric and dimeric forms of the chemokine monocyte chemoattractant protein-1 (MCP-1).
The Journal of biological chemistry 2013;288(14):10024-34.
2013: Emilia Elizabeth Savage; Patrick Michael Sexton; Denise Wootten; Arthur Christopoulos; Sebastian George Barton Furness
A simple method to generate stable cell lines for the analysis of transient protein-protein interactions.
BioTechniques 2013;54(4):217-21.
2013: Denise Wootten; Kyle W Sloop; Francis S Willard; Ana B Bueno; Arthur Christopoulos; Emilia E Savage; Patrick M Sexton
Differential activation and modulation of the glucagon-like peptide-1 receptor by small molecule ligands.
Molecular pharmacology 2013;83(4):822-34.
2013: Denise Wootten; John Simms; Arthur Christopoulos; Laurence J Miller; Patrick M Sexton
Polar transmembrane interactions drive formation of ligand-specific and signal pathway-biased family B G protein-coupled receptor conformations.
Proceedings of the National Academy of Sciences of the United States of America 2013;110(13):5211-6.
2013: Katie Leach; Patrick M Sexton; Adriel Wen; Arthur D Conigrave; Anna E Cook; Arthur Christopoulos
Impact of clinically relevant mutations on the pharmacoregulation and signaling bias of the calcium-sensing receptor by positive and negative allosteric modulators.
Endocrinology 2013;154(3):1105-16.
2013: Cassandra Koole; Laurence J Miller; Kavita Pabreja; Emilia E Savage; Arthur Christopoulos; Sebastian G B Furness; Denise Wootten; Patrick M Sexton
Recent advances in understanding GLP-1R (glucagon-like peptide-1 receptor) function.
Biochemical Society transactions 2013;41(1):172-9.
2013: Alaa Abdul-Ridha; Meritxell Canals; J Robert Lane; Patrick M Sexton; Arthur Christopoulos
Allosteric modulation of a chemogenetically modified G protein-coupled receptor.
Molecular pharmacology 2013;83(2):521-30.
2013: J Robert Lane; Patrick M Sexton; Arthur Christopoulos
Bridging the gap: bitopic ligands of G-protein-coupled receptors.
Trends in pharmacological sciences 2013;34(1):59-66.
2012: Francis S Willard; Denise Wootten; Jorge Alsina-Fernandez; Krister Bokvist; Arthur Christopoulos; Thomas B Farb; James Ficorilli; Sebastian G B Furness; Emilia E Savage; Patrick M Sexton; Aaron D Showalter; Kyle W Sloop
Small molecule allosteric modulation of the glucagon-like Peptide-1 receptor enhances the insulinotropic effect of oxyntomodulin.
Molecular pharmacology 2012;82(6):1066-73.
2012: Karen J Gregory; Patrick M Sexton; Andrew B Tobin; Arthur Christopoulos
Stimulus bias provides evidence for conformational constraints in the structure of a G protein-coupled receptor.
The Journal of biological chemistry 2012;287(44):37066-77.
2012: Denise Wootten; Arthur Christopoulos; James Ficorilli; Lauren T May; Emilia E Savage; Aaron D Showalter; Kyle W Sloop; Celine Valant; Francis S Willard; Patrick M Sexton
Allosteric modulation of endogenous metabolites as an avenue for drug discovery.
Molecular pharmacology 2012;82(2):281-90.
2012: Sebastian G B Furness; Arthur Christopoulos; Denise Wootten; Patrick M Sexton
Consequences of splice variation on Secretin family G protein-coupled receptor function.
British journal of pharmacology 2012;166(1):98-109.
2012: Joshua H Y Tan; Jamie Wedderburn; Deni Taleski; Christopher Boston; Stephen J Butler; Meritxell Canals; Ann Marie Carrick; Arthur Christopoulos; Justin P Ludeman; Todd R Parody; Richard J Payne; Martin J Stone
Design and receptor interactions of obligate dimeric mutant of chemokine monocyte chemoattractant protein-1 (MCP-1).
The Journal of biological chemistry 2012;287(18):14692-702.
2012: Richard J Conway; Ben Capuano; Arthur Christopoulos; Alan D Robertson; Celine Valant; Ian T Crosby
Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6-tetrahydropyridines as 5-HT₂C agonists.
Bioorganic & medicinal chemistry letters 2012;22(7):2560-4.
2012: Celine Valant; Jonathan M White; Patrick M Sexton; Trent D Ashton; Luigi Aurelio; Arthur Christopoulos; Shane M Devine; Peter J Scammells
Synthesis and characterization of novel 2-amino-3-benzoylthiophene derivatives as biased allosteric agonists and modulators of the adenosine A(1) receptor.
Journal of medicinal chemistry 2012;55(5):2367-75.
2012: Anna E Davey; Katie Leach; Patrick M Sexton; Celine Valant; Arthur D Conigrave; Arthur Christopoulos
Positive and negative allosteric modulators promote biased signaling at the calcium-sensing receptor.
Endocrinology 2012;153(3):1232-41.
2012: Cassandra Koole; Laurence J Miller; John Simms; Denise Wootten; Arthur Christopoulos; Patrick M Sexton
Second extracellular loop of human glucagon-like peptide-1 receptor (GLP-1R) has a critical role in GLP-1 peptide binding and receptor activation.
The Journal of biological chemistry 2012;287(6):3642-58.
2012: Cassandra Koole; Laurence J Miller; Emilia E Savage; John Simms; Denise Wootten; Arthur Christopoulos; Patrick M Sexton
Second extracellular loop of human glucagon-like peptide-1 receptor (GLP-1R) differentially regulates orthosteric but not allosteric agonist binding and function.
The Journal of biological chemistry 2012;287(6):3659-73.
2012: Patrick M Sexton; John Simms; Arthur Christopoulos; David R Poyner; Debbie L Hay
RAMPs as drug targets.
Advances in experimental medicine and biology 2012;744():61-74.
2011: Meritxell Canals; Patrick M Sexton; Arthur Christopoulos
Allostery in GPCRs: 'MWC' revisited.
Trends in biochemical sciences 2011;36(12):663-72.
2011: Sanja Bosnyak; Arthur Christopoulos; Emma S Jones; Walter G Thomas; Marie-Isabel Aguilar; Robert E Widdop
Relative affinity of angiotensin peptides and novel ligands at AT1 and AT2 receptors.
Clinical science (London, England : 1979) 2011;121(7):297-303.
2011: Cassandra Koole; Laurence J Miller; John Simms; Celine Valant; Denise Wootten; Arthur Christopoulos; Patrick M Sexton
Polymorphism and ligand dependent changes in human glucagon-like peptide-1 receptor (GLP-1R) function: allosteric rescue of loss of function mutation.
Molecular pharmacology 2011;80(3):486-97.
2011: Luigi Aurelio; Arthur Christopoulos; Bernard L Flynn; Peter J Scammells; Patrick M Sexton; Celine Valant
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.
Bioorganic & medicinal chemistry letters 2011;21(12):3704-7.
2011: Katie Leach; Anna E Davey; Christian C Felder; Patrick M Sexton; Arthur Christopoulos
The role of transmembrane domain 3 in the actions of orthosteric, allosteric, and atypical agonists of the M4 muscarinic acetylcholine receptor.
Molecular pharmacology 2011;79(5):855-65.
2011: S Suratman; K Leach; Pm Sexton; Cc Felder; Re Loiacono; Arthur Christopoulos
Impact of species variability and 'probe-dependence' on the detection and in vivo validation of allosteric modulation at the M4 muscarinic acetylcholine receptor.
British journal of pharmacology 2011;162(7):1659-70.
2011: Geoffrey K Broadhead; Hee-chang Mun; Vimesh A Avlani; Orane Jourdon; W Bret Church; Arthur Christopoulos; Leigh Delbridge; Arthur D Conigrave
Allosteric modulation of the calcium-sensing receptor by gamma-glutamyl peptides: inhibition of PTH secretion, suppression of intracellular cAMP levels, and a common mechanism of action with L-amino acids.
The Journal of biological chemistry 2011;286(11):8786-97.
2011: Katie Leach; Patrick M Sexton; Arthur Christopoulos
Quantification of allosteric interactions at G protein-coupled receptors using radioligand binding assays.
Current protocols in pharmacology / editorial board, S.J. Enna (editor-in-chief) ... [et al.] 2011;Chapter 1():Unit 1.22.
2011: Denise Wootten; John Simms; Cassandra Koole; Owen Woodman; Roger J Summers; Arthur Christopoulos; Patrick M Sexton
Modulation of the glucagon-like peptide-1 receptor signaling by naturally occurring and synthetic flavonoids.
The Journal of pharmacology and experimental therapeutics 2011;336(2):540-50.
2011: Bronwyn A Evans; Natalie Broxton; Jon Merlin; Masaaki Sato; Dana S Hutchinson; Arthur Christopoulos; Roger J Summers
Quantification of functional selectivity at the human α(1A)-adrenoceptor.
Molecular pharmacology 2011;79(2):298-307.
2011: Peter Keov; Patrick M Sexton; Arthur Christopoulos
Allosteric modulation of G protein-coupled receptors: a pharmacological perspective.
Neuropharmacology 2011;60(1):24-35.
2010: Karen J Gregory; Patrick M Sexton; Arthur Christopoulos
Overview of receptor allosterism.
Current protocols in pharmacology / editorial board, S.J. Enna (editor-in-chief) ... [et al.] 2010;Chapter 1():Unit 1.21.
2010: Cassandra Koole; Denise Wootten; John Simms; Celine Valant; Rohan Sridhar; Owen Woodman; Laurence J Miller; Roger J Summers; Arthur Christopoulos; Patrick M Sexton
Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner: implications for drug screening.
Molecular pharmacology 2010;78(3):456-65.
2010: Stephanie A Robinson; Richard E Loiacono; Arthur Christopoulos; Patrick M Sexton; Daniel Malone
The effect of social isolation on rat brain expression of genes associated with endocannabinoid signaling.
Brain research 2010;1343():153-67.
2010: Vimesh A Avlani; Christopher J Langmead; Elizabeth Guida; Martyn D Wood; Ben G Tehan; Hugh J Herdon; Jeannette M Watson; Patrick M Sexton; Arthur Christopoulos
Orthosteric and allosteric modes of interaction of novel selective agonists of the M1 muscarinic acetylcholine receptor.
Molecular pharmacology 2010;78(1):94-104.
2010: Vindhya Nawaratne; Katie Leach; Christian Felder; Patrick M Sexton; Arthur Christopoulos
Structural determinants of allosteric agonism and modulation at the M4 muscarinic acetylcholine receptor: identification of ligand-specific and global activation mechanisms.
The Journal of biological chemistry 2010;285(25):19012-21.
2010: Karen J Gregory; Nathan E Hall; Andrew B Tobin; Patrick M Sexton; Arthur Christopoulos
Identification of orthosteric and allosteric site mutations in M2 muscarinic acetylcholine receptors that contribute to ligand-selective signaling bias.
The Journal of biological chemistry 2010;285(10):7459-74.
2010: Katie Leach; Richard E Loiacono; Christian Felder; David L McKinzie; Adrian Mogg; David B Shaw; Patrick M Sexton; Arthur Christopoulos
Molecular mechanisms of action and in vivo validation of an M4 muscarinic acetylcholine receptor allosteric modulator with potential antipsychotic properties.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology 2010;35(4):855-69.
2010: Denise L Wootten; John Simms; Debbie L Hay; Arthur Christopoulos; Patrick M Sexton
Receptor activity modifying proteins and their potential as drug targets.
Progress in molecular biology and translational science 2010;91():53-79.
2009: Luigi Aurelio; Celine Valant; Heidi Figler; Bernard L Flynn; Joel Linden; Patrick M Sexton; Arthur Christopoulos; Peter J Scammells
3- and 6-Substituted 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridines as A1 adenosine receptor allosteric modulators and antagonists.
Bioorganic & medicinal chemistry 2009;17(20):7353-61.
2009: Luigi Aurelio; Celine Valant; Bernard L Flynn; Patrick M Sexton; Arthur Christopoulos; Peter J Scammells
Allosteric modulators of the adenosine A1 receptor: synthesis and pharmacological evaluation of 4-substituted 2-amino-3-benzoylthiophenes.
Journal of medicinal chemistry 2009;52(14):4543-7.
2009: Celine Valant; Patrick M Sexton; Arthur Christopoulos
Orthosteric/allosteric bitopic ligands: going hybrid at GPCRs.
Molecular interventions 2009;9(3):125-35.
2009: Patrick M Sexton; David R Poyner; John Simms; Arthur Christopoulos; Debbie L Hay
Modulating receptor function through RAMPs: can they represent drug targets in themselves?
Drug discovery today 2009;14(7-8):413-9.
2009: John Simms; Nathan E Hall; Polo H C Lam; Laurence J Miller; Arthur Christopoulos; Ruben Abagyan; Patrick M Sexton
Homology modeling of GPCRs.
Methods in molecular biology (Clifton, N.J.) 2009;552():97-113.
2008: Tim Werry; Gregory D Stewart; Michael F Crouch; Anne Watts; Patrick M Sexton; Arthur Christopoulos
Pharmacology of 5HT(2C) receptor-mediated ERK1/2 phosphorylation: agonist-specific activation pathways and the impact of RNA editing.
Biochemical pharmacology 2008;76(10):1276-87.
2008: Maria Morfis; Nanda Tilakaratne; Sebastian G B Furness; George Christopoulos; Tim Werry; Arthur Christopoulos; Patrick M Sexton
Receptor activity-modifying proteins differentially modulate the G protein-coupling efficiency of amylin receptors.
Endocrinology 2008;149(11):5423-31.
2008: Vindhya Nawaratne; Katie Leach; Nur Suratman; Richard E Loiacono; Christian Felder; Blaine N Armbruster; Bryan L Roth; Patrick M Sexton; Arthur Christopoulos
New insights into the function of M4 muscarinic acetylcholine receptors gained using a novel allosteric modulator and a DREADD (designer receptor exclusively activated by a designer drug).
Molecular pharmacology 2008;74(4):1119-31.
2008: Tao Qi; George Christopoulos; Richard J Bailey; Arthur Christopoulos; Patrick M Sexton; Debbie L Hay
Identification of N-terminal receptor activity-modifying protein residues important for calcitonin gene-related peptide, adrenomedullin, and amylin receptor function.
Molecular pharmacology 2008;74(4):1059-71.
2008: Tim Werry; Richard E Loiacono; Patrick M Sexton; Arthur Christopoulos
RNA editing of the serotonin 5HT2C receptor and its effects on cell signalling, pharmacology and brain function.
Pharmacology & therapeutics 2008;119(1):7-23.
2008: Vimesh A Avlani; David J McLoughlin; Patrick M Sexton; Arthur Christopoulos
The impact of orthosteric radioligand depletion on the quantification of allosteric modulator interactions.
The Journal of pharmacology and experimental therapeutics 2008;325(3):927-34.
2008: Patrick M Sexton; George Christopoulos; Arthur Christopoulos; Eric S Nylen; Richard H Snider; Kenneth L Becker
Procalcitonin has bioactivity at calcitonin receptor family complexes: potential mediator implications in sepsis.
Critical care medicine 2008;36(5):1637-40.
2008: Madhara Udawela; George Christopoulos; Maria Morfis; Nanda Tilakaratne; Arthur Christopoulos; Patrick M Sexton
The effects of C-terminal truncation of receptor activity modifying proteins on the induction of amylin receptor phenotype from human CTb receptors.
Regulatory peptides 2008;145(1-3):65-71.
2007: Karen J Gregory; Patrick M Sexton; Arthur Christopoulos
Allosteric modulation of muscarinic acetylcholine receptors.
Current neuropharmacology 2007;5(3):157-67.
2007: J Espallergues; P Lapalud; Arthur Christopoulos; Vimesh A Avlani; Patrick M Sexton; A Vamvakides; Tangui Maurice
Involvement of the sigma1 (sigma1) receptor in the anti-amnesic, but not antidepressant-like, effects of the aminotetrahydrofuran derivative ANAVEX1-41.
British journal of pharmacology 2007;152(2):267-79.
2007: Vimesh A Avlani; Karen J Gregory; Craig J Morton; Michael W Parker; Patrick M Sexton; Arthur Christopoulos
Critical role for the second extracellular loop in the binding of both orthosteric and allosteric G protein-coupled receptor ligands.
The Journal of biological chemistry 2007;282(35):25677-86.
2007: Katie Leach; Patrick M Sexton; Arthur Christopoulos
Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology.
Trends in pharmacological sciences 2007;28(8):382-9.
2007: Lauren T May; Vimesh A Avlani; Christopher J Langmead; Hugh J Herdon; Martyn D Wood; Patrick M Sexton; Arthur Christopoulos
Structure-function studies of allosteric agonism at M2 muscarinic acetylcholine receptors.
Molecular pharmacology 2007;72(2):463-76.
2007: Lauren T May; Katie Leach; Patrick M Sexton; Arthur Christopoulos
Allosteric modulation of G protein-coupled receptors.
Annual review of pharmacology and toxicology 2007;47():1-51.
2006: Debbie L Hay; George Christopoulos; Arthur Christopoulos; Patrick M Sexton
Determinants of 1-piperidinecarboxamide, N-[2-[[5-amino-l-[[4-(4-pyridinyl)-l-piperazinyl]carbonyl]pentyl]amino]-1-[(3,5-dibromo-4-hydroxyphenyl)methyl]-2-oxoethyl]-4-(1,4-dihydro-2-oxo-3(2H)-quinazolinyl) (BIBN4096BS) affinity for calcitonin gene-related peptide and amylin receptors--the role of receptor activity modifying protein 1.
Molecular pharmacology 2006;70(6):1984-91.
2006: Madhara Udawela; George Christopoulos; Maria Morfis; Arthur Christopoulos; Siying Ye; Nanda Tilakaratne; Patrick M Sexton
A critical role for the short intracellular C terminus in receptor activity-modifying protein function.
Molecular pharmacology 2006;70(5):1750-60.
2006: Christopher J Langmead; Arthur Christopoulos
Allosteric agonists of 7TM receptors: expanding the pharmacological toolbox.
Trends in pharmacological sciences 2006;27(9):475-81.
2006: Alfred A Lanzafame; Patrick M Sexton; Arthur Christopoulos
Interaction studies of multiple binding sites on m4 muscarinic acetylcholine receptors.
Molecular pharmacology 2006;70(2):736-46.
2006: Patrick M Sexton; Maria Morfis; Nanda Tilakaratne; Debbie L Hay; Madhara Udawela; George Christopoulos; Arthur Christopoulos
Complexing receptor pharmacology: modulation of family B G protein-coupled receptor function by RAMPs.
Annals of the New York Academy of Sciences 2006;1070():90-104.
2006: Madhara Udawela; George Christopoulos; Nanda Tilakaratne; Arthur Christopoulos; Anthony L Albiston; Patrick M Sexton
Distinct receptor activity-modifying protein domains differentially modulate interaction with calcitonin receptors.
Molecular pharmacology 2006;69(6):1984-9.
2006: Tim Werry; Arthur Christopoulos; Patrick M Sexton
Mechanisms of ERK1/2 regulation by seven-transmembrane-domain receptors.
Current pharmaceutical design 2006;12(14):1683-702.
2006: Christopher J Langmead; Victoria A H Fry; Ian T Forbes; Clive L Branch; Arthur Christopoulos; Martyn D Wood; Hugh J Herdon
Probing the molecular mechanism of interaction between 4-n-butyl-1-[4-(2-methylphenyl)-4-oxo-1-butyl]-piperidine (AC-42) and the muscarinic M(1) receptor: direct pharmacological evidence that AC-42 is an allosteric agonist.
Molecular pharmacology 2006;69(1):236-46.
2005: Lauren T May; Patrick M Sexton; Arthur Christopoulos
Effects of urea pretreatment on the binding properties of adenosine A1 receptors.
British journal of pharmacology 2005;146(8):1119-29.
2005: Tim Werry; Karen J Gregory; Patrick M Sexton; Arthur Christopoulos
Characterization of serotonin 5-HT2C receptor signaling to extracellular signal-regulated kinases 1 and 2.
Journal of neurochemistry 2005;93(6):1603-15.
2005: Debbie L Hay; George Christopoulos; Arthur Christopoulos; David R Poyner; Patrick M Sexton
Pharmacological discrimination of calcitonin receptor: receptor activity-modifying protein complexes.
Molecular pharmacology 2005;67(5):1655-65.
2005: Dana S Hutchinson; Masaaki Sato; Bronwyn A Evans; Arthur Christopoulos; Roger J Summers
Evidence for pleiotropic signaling at the mouse beta3-adrenoceptor revealed by SR59230A [3-(2-Ethylphenoxy)-1-[(1,S)-1,2,3,4-tetrahydronapth-1-ylamino]-2S-2-propanol oxalate].
The Journal of pharmacology and experimental therapeutics 2005;312(3):1064-74.
2005: Tim Werry; Patrick M Sexton; Arthur Christopoulos
"Ins and outs" of seven-transmembrane receptor signalling to ERK.
Trends in endocrinology and metabolism: TEM 2005;16(1):26-33.
2005: Lauren T May; Yvonne Lin; Patrick M Sexton; Arthur Christopoulos
Regulation of M2 muscarinic acetylcholine receptor expression and signaling by prolonged exposure to allosteric modulators.
The Journal of pharmacology and experimental therapeutics 2005;312(1):382-90.
2004: Alfred A Lanzafame; Elizabeth Guida; Arthur Christopoulos
Effects of anandamide on the binding and signaling properties of M1 muscarinic acetylcholine receptors.
Biochemical pharmacology 2004;68(11):2207-19.
2004: Arthur Christopoulos; Lauren T May; Vimesh A Avlani; Patrick M Sexton
G-protein-coupled receptor allosterism: the promise and the problem(s).
Biochemical Society transactions 2004;32(Pt 5):873-7.
2004: Debbie L Hay; George Christopoulos; Arthur Christopoulos; Patrick M Sexton
Amylin receptors: molecular composition and pharmacology.
Biochemical Society transactions 2004;32(Pt 5):865-7.
2004: Mark G Devlin; Nicola J Smith; Olivia M Ryan; Elizabeth Guida; Patrick M Sexton; Arthur Christopoulos
Regulation of serotonin 5-HT2C receptors by chronic ligand exposure.
European journal of pharmacology 2004;498(1-3):59-69.
2004: Vimesh A Avlani; Lauren T May; Patrick M Sexton; Arthur Christopoulos
Application of a kinetic model to the apparently complex behavior of negative and positive allosteric modulators of muscarinic acetylcholine receptors.
The Journal of pharmacology and experimental therapeutics 2004;308(3):1062-72.
2004: Alfred A Lanzafame; Arthur Christopoulos
Investigation of the interaction of a putative allosteric modulator, N-(2,3-diphenyl-1,2,4-thiadiazole-5-(2H)-ylidene) methanamine hydrobromide (SCH-202676), with M1 muscarinic acetylcholine receptors.
The Journal of pharmacology and experimental therapeutics 2004;308(3):830-7.
2004: Lauren T May; Vimesh A Avlani; Patrick M Sexton; Arthur Christopoulos
Allosteric modulation of G protein-coupled receptors.
Current pharmaceutical design 2004;10(17):2003-13.
2003: Richard Neubig; Michael Spedding; Terry Kenakin; Arthur Christopoulos
International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification. XXXVIII. Update on terms and symbols in quantitative pharmacology.
Pharmacological reviews 2003;55(4):597-606.
2003: Maria Morfis; Arthur Christopoulos; Patrick M Sexton
RAMPs: 5 years on, where to now?
Trends in pharmacological sciences 2003;24(11):596-601.
2003: Lauren T May; Arthur Christopoulos
Allosteric modulators of G-protein-coupled receptors.
Current opinion in pharmacology 2003;3(5):551-6.
2003: Arthur Christopoulos; George Christopoulos; Maria Morfis; Madhara Udawela; Marc Laburthe; Alain Couvineau; Kenji Kuwasako; Nanda Tilakaratne; Patrick M Sexton
Novel receptor partners and function of receptor activity-modifying proteins.
The Journal of biological chemistry 2003;278(5):3293-7.
2003: Alfred A Lanzafame; Arthur Christopoulos; Frederick Mitchelson
Cellular signaling mechanisms for muscarinic acetylcholine receptors.
Receptors & channels 2003;9(4):241-60.
2002: Arthur Christopoulos; Terry Kenakin
G protein-coupled receptor allosterism and complexing.
Pharmacological reviews 2002;54(2):323-74.
2002: Arthur Christopoulos
Allosteric binding sites on cell-surface receptors: novel targets for drug discovery.
Nature reviews. Drug discovery 2002;1(3):198-210.
2002: Mark G Devlin; Arthur Christopoulos
Modulation of cannabinoid agonist binding by 5-HT in the rat cerebellum.
Journal of neurochemistry 2002;80(6):1095-102.
2001: Michael J Lew; Arthur Christopoulos; James Ziogas
Insurmountable AT1 receptor antagonism: message in a model?
Trends in pharmacological sciences 2001;22(11):555-7.
2001: Arthur Christopoulos; K Wilson
Interaction of anandamide with the M(1) and M(4) muscarinic acetylcholine receptors.
Brain research 2001;915(1):70-8.
2001: Arthur Christopoulos; Marianne K O Grant; N Ayoubzadeh; O N Kim; Per Sauerberg; Lone Jeppesen; Esam E El-Fakahany
Synthesis and pharmacological evaluation of dimeric muscarinic acetylcholine receptor agonists.
The Journal of pharmacology and experimental therapeutics 2001;298(3):1260-8.
2001: Alfred A Lanzafame; Arthur Christopoulos; Frederick Mitchelson
The allosteric interaction of otenzepad (AF-DX 116) at muscarinic M2 receptors in guinea pig atria.
European journal of pharmacology 2001;416(3):235-44.
2001: Arthur Christopoulos; P Coles; L Lay; Michael J Lew; James A Angus
Pharmacological analysis of cannabinoid receptor activity in the rat vas deferens.
British journal of pharmacology 2001;132(6):1281-91.
2001: Arthur Christopoulos
From 'captive' agonism to insurmountable antagonism: demonstrating the power of analytical pharmacology.
Clinical and experimental pharmacology & physiology 2001;28(3):223-9.
2000: Michael J Lew; James Ziogas; Arthur Christopoulos
Dynamic mechanisms of non-classical antagonism by competitive AT(1) receptor antagonists.
Trends in pharmacological sciences 2000;21(10):376-81.
2000: Ahmet Akici; Atila Karaalp; Ece ISkender; Arthur Christopoulos; Esam E El-Fakahany; Sule Oktay
Further evidence for the heterogeneity of functional muscarinic receptors in guinea pig gallbladder.
European journal of pharmacology 2000;388(1):115-23.
2000: Arthur Christopoulos; Marianne K O Grant; Esam E El-Fakahany
Transducer abstraction: a novel approach to the detection of partial agonist efficacy in radioligand binding studies.
Journal of pharmacological and toxicological methods 2000;43(1):55-67.
1999: Arthur Christopoulos; AM Parsons; Michael J Lew; Esam E El-Fakahany
The assessment of antagonist potency under conditions of transient response kinetics.
European journal of pharmacology 1999;382(3):217-27.
1999: Arthur Christopoulos; Esam E El-Fakahany
Qualitative and quantitative assessment of relative agonist efficacy.
Biochemical pharmacology 1999;58(5):735-48.
1999: Marianne K O Grant; Arthur Christopoulos; Esam E El-Fakahany
Regulation of acetylcholine binding by ATP at the muscarinic M(1) receptor in intact CHO cells.
Brain research 1999;839(1):94-9.
1999: Arthur Christopoulos; AM Parsons; Esam E El-Fakahany
Pharmacological analysis of the novel mode of interaction between xanomeline and the M1 muscarinic acetylcholine receptor.
The Journal of pharmacology and experimental therapeutics 1999;289(3):1220-8.
1999: Arthur Christopoulos; JL Sorman; Frederick Mitchelson; Esam E El-Fakahany
Characterization of the subtype selectivity of the allosteric modulator heptane-1,7-bis-(dimethyl-3'-phthalimidopropyl) ammonium bromide (C7/3-phth) at cloned muscarinic acetylcholine receptors.
Biochemical pharmacology 1999;57(2):171-9.
1999: Arthur Christopoulos; Esam E El-Fakahany
The generation of nitric oxide by G protein-coupled receptors.
Life sciences 1999;64(1):1-15.
1998: Arthur Christopoulos; Frederick Mitchelson
Use of a spreadsheet to quantitate the equilibrium binding of an allosteric modulator.
European journal of pharmacology 1998;355(1):103-11.
1998: Arthur Christopoulos; T L Pierce; JL Sorman; Esam E El-Fakahany
On the unique binding and activating properties of xanomeline at the M1 muscarinic acetylcholine receptor.
Molecular pharmacology 1998;53(6):1120-30.
1998: Arthur Christopoulos; Alfred A Lanzafame; Frederick Mitchelson
Allosteric interactions at muscarinic cholinoceptors.
Clinical and experimental pharmacology & physiology 1998;25(3-4):185-94.
1997: Arthur Christopoulos; Frederick Mitchelson
Pharmacological analysis of the mode of interaction of McN-A-343 at atrial muscarinic M2 receptors.
European journal of pharmacology 1997;339(2-3):153-6.
1997: Arthur Christopoulos; Esam E El-Fakahany
Novel persistent activation of muscarinic M1 receptors by xanomeline.
European journal of pharmacology 1997;334(1):R3-4.
1997: Arthur Christopoulos; Frederick Mitchelson
Application of an allosteric ternary complex model to the technique of pharmacological resultant analysis.
The Journal of pharmacy and pharmacology 1997;49(8):781-6.
1997: Alfred A Lanzafame; Arthur Christopoulos; Frederick Mitchelson
Three allosteric modulators act at a common site, distinct from that of competitive antagonists, at muscarinic acetylcholine M2 receptors.
The Journal of pharmacology and experimental therapeutics 1997;282(1):278-85.
1997: Arthur Christopoulos; Alfred A Lanzafame; A Ziegler; Frederick Mitchelson
Kinetic studies of co-operativity at atrial muscarinic M2 receptors with an "infinite dilution" procedure.
Biochemical pharmacology 1997;53(6):795-800.
1997: Anwarul Hassan Gilani; F Shaheen; Arthur Christopoulos; Frederick Mitchelson
Interaction of ebeinone, an alkaloid from Fritillaria imperialis, at two muscarinic acetylcholine receptor subtypes.
Life sciences 1997;60(8):535-44.
1996: Alfred A Lanzafame; Arthur Christopoulos; Frederick Mitchelson
Interactions of agonists with an allosteric antagonist at muscarinic acetylcholine M2 receptors.
European journal of pharmacology 1996;316(1):27-32.
1995: Arthur Christopoulos; Frederick Mitchelson
[3H]N-methylscopolamine dissociation from muscarine receptors affected by low concentrations of allosteric modulators.
European journal of pharmacology 1995;290(3):259-62.
1994: Arthur Christopoulos; Frederick Mitchelson
Assessment of the allosteric interactions of the bisquaternary heptane-1,7-bis(dimethyl-3'-phthalimidopropyl)ammonium bromide at M1 and M2 muscarine receptors.
Molecular pharmacology 1994;46(1):105-14.
1993: Arthur Christopoulos; R Loiacono; Frederick Mitchelson
Binding of the muscarine receptor antagonist heptane-1,7-bis(dimethyl-3'-phthalimidopropyl)ammonium bromide at cholinoceptor sites.
European journal of pharmacology 1993;246(1):1-8.