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Research Output 1993 2019

2009

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

Sexton, P. M., Poyner, D. R., Simms, J. W., Christopoulos, A. & Hay, D. L., 2009, In : Drug Discovery Today. 14, 7-8, p. 413 - 419 7 p.

Research output: Contribution to journalArticleResearchpeer-review

Orthosteric/allosteric bitopic ligands going hybrid with GPCRs

Valant, C., Sexton, P. M. & Christopoulos, A., 1 Jun 2009, In : Molecular Interventions. 9, 3, p. 125-135 11 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

2008

2-Aminothienopyridazines as novel adenosine A1 receptor allosteric modulators and antagonists

Ferguson, G. N., Valant, C., Horne, H. J., Figler, H., Flynn, B. L., Linden, J., Chalmers, D. K., Sexton, P., Christopoulos, A. & Scammells, P. J., 2008, In : Journal of Medicinal Chemistry. 51, 19, p. 6165 - 6172 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Allosteric modulation of the muscarinic M4 receptor as an approach to treating schizophrenia

Chan, W. Y., McKinzie, D. L., Bose, S., Mitchell, S. N., Witkin, J. M., Thompson, R. C., Christopoulos, A., Lazareno, S., Birdsall, N. JM., Bymaster, F. P. & Felder, C. C., 2008, In : Proceedings of the National Academy of Sciences. 105, 31, p. 10978 - 10983 6 p.

Research output: Contribution to journalArticleResearchpeer-review

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

Gao, F., Sexton, P., Christopoulos, A. & Miller, L. J., 2008, In : Bioorganic and Medicinal Chemistry Letters. 18, 5, p. 4401 - 4404 4 p.

Research output: Contribution to journalArticleResearchpeer-review

Identification of N-terminal receptor activity-modifying protein residues important for calcitonin gene-related peptide, adrenomedullin, and amylin receptor function

Qi, T., Christopoulos, G., Bailey, R. J., Christopoulos, A., Sexton, P. & Hay, D. L., 2008, In : Molecular Pharmacology. 74, 4, p. 1059 - 1071 13 p.

Research output: Contribution to journalArticleResearchpeer-review

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)

Nawaratne, O. V., Leach, K., Suratman, S., Loiacono, R., Felder, C. C., Armbruster, B. N., Roth, B. L., Sexton, P. & Christopoulos, A., 2008, In : Molecular Pharmacology. 74, 4, p. 1119 - 1131 13 p.

Research output: Contribution to journalArticleResearchpeer-review

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

Werry, T. D., Stewart, G. D., Crouch, M. F., Watts, A., Sexton, P. & Christopoulos, A., 2008, In : Biochemical Pharmacology. 76, 10, p. 1276 - 1287 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Procalcitonin has bioactivity at calcitonin receptor family complexes: Potential mediator implications in sepsis

Sexton, P., Christopoulos, G., Christopoulos, A., Nylen, E. S., Snider Jr., R. H. & Becker, K. L., 2008, In : Critical Care Medicine. 36, 5, p. 1637 - 1640 4 p.

Research output: Contribution to journalArticleResearchpeer-review

Receptor activity-modifying proteins differentially modulate the G protein-coupling efficiency of amylin receptors

Morfis, M., Tilakaratne, N., Furness, S. G. B., Christopoulos, G., Werry, T. D., Christopoulos, A. & Sexton, P., 2008, In : Endocrinology. 149, 11, p. 5423 - 5431 9 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File

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

Werry, T. D., Loiacono, R., Sexton, P. & Christopoulos, A., 2008, In : Pharmacology and Therapeutics. 119, 1, p. 7 - 23 17 p.

Research output: Contribution to journalArticleResearchpeer-review

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

Moloney, G. P., Angus, J. A., Robertson, A. D., Stoermer, M. J., Robinson, M. S., Wright, C. E., McRae, K. & Christopoulos, A., 2008, In : European Journal of Medicinal Chemistry. 43, 1, p. 513 - 539 26 p.

Research output: Contribution to journalArticleResearchpeer-review

Synthesis and cannabinoid activity of a variety of 2,3-substituted 1-benzo[b]thiophen derivatives and 2,3-substituted benzofuran: Novel agonists for the CB1 receptor

Moloney, G. P., Angus, J. A., Robertson, A. D., Stoermer, M. J., Robinson, M., Lay, L., Wright, C. E., McRae, K. & Christopoulos, A., 28 Jul 2008, In : Australian Journal of Chemistry. 61, 7, p. 484-499 16 p.

Research output: Contribution to journalArticleResearchpeer-review

The effects of C-terminal truncation of receptor activity modifying proteins on the induction of amylin receptor phenotype from human CTb receptors

Udawela, M., Christopoulos, G., Morfis, M., Tilakaratne, N., Christopoulos, A. & Sexton, P., 2008, In : Regulatory Peptides. 145, p. 65 - 71 6 p.

Research output: Contribution to journalArticleResearchpeer-review

The impact of orthosteric radioligand depletion on the quantification of allosteric modulator interactions

Avlani, V. A., McLoughlin, D. J., Sexton, P. & Christopoulos, A., 2008, In : Journal of Pharmacology and Experimental Therapeutics. 325, 3, p. 927 - 934 8 p.

Research output: Contribution to journalArticleResearchpeer-review

2007

Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology

Leach, K., Sexton, P. & Christopoulos, A., 2007, In : Trends in Pharmacological Sciences. 28, 8, p. 382 - 389 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Allosteric modulation of G protein-coupled receptors

May, L. T., Leach, K., Sexton, P. M. & Christopoulos, A., 2007, In : Annual Review of Pharmacology and Toxicology. 47, p. 1 - 51 51 p.

Research output: Contribution to journalArticleResearchpeer-review

Allosteric modulation of muscarinic acetylcholine receptors

Gregory, K. J., Sexton, P. & Christopoulos, A., 2007, In : Current Neuropharmacology. 5, 3, p. 157 - 167 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Critical role for the second extracellular loop in the binding of both orthosteric and allosteric G protein-coupled receptor ligands

Avlani, V. A., Gregory, K. J., Morton, C. J., Parker, M. W., Sexton, P. & Christopoulos, A., 2007, In : Journal of Biological Chemistry. 282, 35, p. 25677 - 25686 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs

Bisson, W. H., Cheltsov, A. V., Bruey-Sedano, N., Lin, B., Chen, J., Goldberger, N., May, L. T., Christopoulos, A., Dalton, J. T., Sexton, P., Zhang, X-K. & Abagyan, R., 2007, In : Proceedings of the National Academy of Sciences. 104, 29, p. 11927 - 11932 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Functional selectivity and classical concepts of quantitative pharmacology

Urban, J. D., Clarke, W. P., von Zastrow, M., Nichols, D. E., Kobilka, B., Weinstein, H., Javitch, J. A., Roth, B. L., Christopoulos, A., Sexton, P. M., Miller, K. J., Spedding, M. & Mailman, R. B., 2007, In : Journal of Pharmacology and Experimental Therapeutics. 320, 1, p. 1 - 13 13 p.

Research output: Contribution to journalArticleResearchpeer-review

History of research on nicotinic and muscarinic cholinergic receptors

Karczmar, A. G., Lindstrom, J. & Christopoulos, A., 2007, Exploring the Vertebrate Central Cholinergic Nervous System. Karczmar, A. G. (ed.). First ed. New York USA: Springer, p. 151 - 162 12 p.

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Other

Involvement of the sigma1 (sigma1) receptor in the anti-amnesic, but not antidepressant-like, effects of the aminotetrahydrofuran derivative ANAVEX1-41

Espallergues, J., Lapalud, P., Christopoulos, A., Avlani, V. A., Sexton, P., Vamvakides, A. & Maurice, T., 2007, In : British Journal of Pharmacology. 152, 2, p. 267 - 279 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Muscarinic acetylcholine receptors in the central nervous system: structure, function and pharmacology

Christopoulos, A., 2007, Exploring the Vertebrate Central Cholinergic Nervous System. Karczmar, A. G. (ed.). First ed. New York USA: Springer, p. 163 - 208 46 p.

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Researchpeer-review

Structure-function studies of allosteric agonism at M2 muscarinic acetylcholine receptors

May, L. T., Avlani, V. A., Langmead, C. J., Herdon, H. J., Wood, M. D., Sexton, P. & Christopoulos, A., 2007, In : Molecular Pharmacology. 72, 2, p. 463 - 476 14 p.

Research output: Contribution to journalArticleResearchpeer-review

2006

A critical role for the short intracellular C terminus in receptor activity-modifying protein function

Udawela, M., Christopoulos, G., Morfis, M., Christopoulos, A., Ye, S., Tilakaratne, N. & Sexton, P. M., 2006, In : Molecular Pharmacology. 70, 5, p. 1750 - 1760 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Allosteric agonists of 7TM receptors: expanding the pharmacological toolbox

Langmead, C. J. & Christopoulos, A., 2006, In : Trends in Pharmacological Sciences. 27, 9, p. 475 - 481 7 p.

Research output: Contribution to journalArticleResearchpeer-review

Complexing receptor pharmacology: modulation of family B G protein-coupled receptor function by RAMPs

Sexton, P., Morfis, M., Tilakaratne, N., Hay, D. L., Udawela, M., Christopoulos, G. & Christopoulos, A., 2006, In : Annals of the New York Academy of Sciences. 1070, p. 90 - 104 15 p.

Research output: Contribution to journalArticleResearchpeer-review

Distinct receptor activity-modifying protein domains differentially modulate interaction with calcitonin receptors

Udawela, M., Christopoulos, G., Tilakaratne, N., Christopoulos, A., Albiston, A. L. & Sexton, P. M., 2006, In : Molecular Pharmacology. 69, 6, p. 1984 - 1989 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Effective GPCR screening using ERK 1/2: applying SureFire to detect ERK 1/2 phosphorylation

Osmond, R. W., Dyer, A. R., Sexton, P. M., Christopoulos, A. & Crouch, M. F., 2006, In : Genetic Engineering News. 26, 1, p. 27 - 28 2 p.

Research output: Contribution to journalArticleResearchpeer-review

GPCR allosterism: A novel approach to drug selectivity

Christopoulos, A., 2006, p. 9 - 9. 1 p.

Research output: Contribution to conferenceAbstractOther

G protein-coupled receptor drug targets

Sexton, P. M. & Christopoulos, A., 2006, In : Current Pharmaceutical Design. 12, 14, p. 1681 - 1682 2 p.

Research output: Contribution to journalLetterOther

Interaction studies of multiple binding sites on M4 muscarinic acetylcholine receptors

Lanzafame, A. A., Sexton, P. M. & Christopoulos, A., 2006, In : Molecular Pharmacology. 70, 2, p. 736 - 746 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Mechanisms of ERK1/2 regulation by seven-transmembrane-domain receptors

Werry, T. D., Christopoulos, A. & Sexton, P. M., 2006, In : Current Pharmaceutical Design. 12, 14, p. 1683 - 1702 20 p.

Research output: Contribution to journalArticleResearchpeer-review

Non-classical modes of signaling by 5HT(2C) receptors

Christopoulos, A., 2006, p. 55 - 55. 1 p.

Research output: Contribution to conferenceAbstractOther

On the mechanism of interaction of potent surmountable and insurmountable antagonists with the prostaglandin D2 receptor CRTH2

Mathiesen, J. M., Christopoulos, A., Ulven, T., Royer, J. F., Campillo, M., Heinemann, A., Pardo, L. & Kostenis, E., 2006, In : Molecular Pharmacology. 69, 4, p. 1441 - 1453 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Probing the molecular mechanism of interaction between 4-n-butyl-1-[4-(2- methylphenyl)-4-oxo-1-butyl]-piperidine (AC-42) and the muscarinic M1 receptor: Direct pharmacological evidence that AC-42 is an allosteric agonist

Langmead, C. J., Fry, V. A., Forbes, I. T., Branch, C. L., Christopoulos, A., Wood, M. D. & Herdon, H. J., 2006, In : Molecular Pharmacology. 69, 1, p. 236 - 246 11 p.

Research output: Contribution to journalArticleResearchpeer-review

2005

Allosteric modulation of the cannabinoid CB1 receptor

Price, M. R., Baillie, G. L., Thomas, A., Stevenson, L. A., Easson, M., Goodwin, R., McLean, A., McIntosh, L., Goodwin, G., Walker, G., Westwood, P., Marrs, J., Thomson, F., Cowley, P., Christopoulos, A., Pertwee, R. G. & Ross, R. A., 2005, In : Molecular Pharmacology. 68, 5, p. 1484 - 1495 12 p.

Research output: Contribution to journalArticleResearchpeer-review

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

Werry, T. D., Gregory, K. J., Sexton, P. M. & Christopoulos, A., 2005, In : Journal of Neurochemistry. 93, p. 1603 - 1615 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Editorial

Christopoulos, A., 1 Jun 2005, In : Mini-Reviews in Medicinal Chemistry. 5, 6, p. 521-521 1 p.

Research output: Contribution to journalEditorialOtherpeer-review

Effects of urea pretreatment on the binding properties of adenosine A 1 receptors

May, L. T., Sexton, P. M. & Christopoulos, A., 2005, In : British Journal of Pharmacology. 146, 8, p. 1119 - 1129 11 p.

Research output: Contribution to journalArticleResearchpeer-review

G-protein-coupled receptor Mas is a physiological antagonist of the angiotensin II type 1 receptor

Kostenis, E., Milligan, G., Christopoulos, A., Sanchez-Ferrer, C. F., Heringer-Walther, S., Sexton, P. M., Gembardt, F., Kellett, E., Martini, L., Vanderheyden, P., Schultheiss, H-P. & Walther, T., 2005, In : Circulation. 111, p. 1806 - 1813 8 p.

Research output: Contribution to journalArticleResearchpeer-review

'Ins and outs' of seven-transmembrane receptor signalling to ERK

Werry, T. D., Sexton, P. M. & Christopoulos, A., 2005, In : Trends in Endocrinology and Metabolism. 16, 1, p. 26 - 33 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Pharmacological discrimination of calcitonin receptor: receptor activity-modifying protein complexes

Hay, D. L., Christopoulos, G., Christopoulos, A., Poyner, D. R. & Sexton, P. M., 2005, In : Molecular Pharmacology. 67, 5, p. 1655 - 1665 11 p.

Research output: Contribution to journalArticleResearchpeer-review

2004

Allosteric modulation of G protein-coupled receptors

May, L. T., Avlani, V. A., Sexton, P. & Christopoulos, A., 2004, In : Current Pharmaceutical Design. 10, 17, p. 2003 - 2013 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Allosteric modulation of G protein-coupled receptors

May, L. T., Avlani, V. A., Sexton, P. M. & Christopoulos, A., 2004, In : Current Pharmaceutical Design. 10, 17, p. 2003-2013 11 p.

Research output: Contribution to journalReview ArticleResearchpeer-review