1993 …2023
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Research Output 1993 2019

2010

Second Messenger Assays for G Protein-Coupled Receptors: cAMP, Ca2+, Inositol Phosphates, ERK1/2

Gregory, K. J., Sexton, P. M., Christopoulos, A. & Hick, C. A., 25 Jan 2010, G Protein-Coupled Receptors: Essential Methods. Wiley-Blackwell, p. 31-52 22 p.

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

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

Robinson, S. A., Loiacono, R., Christopoulos, A., Sexton, P. & Malone, D. T., 2010, In : Brain Research. 1343, p. 153 - 167 15 p.

Research output: Contribution to journalArticleResearchpeer-review

The Emergence of Allosteric Modulators for G Protein-Coupled Receptors

Gregory, K. J., Valant, C., Simms, J., Sexton, P. M. & Christopoulos, A., 15 Jul 2010, GPCR Molecular Pharmacology and Drug Targeting: Shifting Paradigms and New Directions. John Wiley & Sons, p. 61-87 27 p.

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

Understanding amylin Receptors

Just, R., Simms, J., Furness, S. G. B., Christopoulos, A. & Sexton, P. M., 2010, The Calcitonin Gene-related Peptide Family: Form, Function and Future Perspectives. Springer, p. 41-57 17 p.

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

2009

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

Aurelio, L., Valant, C., Figler, H., Flynn, B. L., Linden, J., Sexton, P., Christopoulos, A. & Scammells, P. J., 2009, In : Bioorganic & Medicinal Chemistry. 17, 20, p. 7353 - 7361 9 p.

Research output: Contribution to journalArticleResearchpeer-review

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

Conn, P. J., Christopoulos, A. & Lindsley, C. W., 2009, In : Nature Reviews Drug Discovery. 8, 1, p. 41 - 54 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa

Mansfield, K. J., Chandran, J. J., Vaux, K. J., Millard, R. J., Christopoulos, A., Mitchelson, F. J. & Burcher, E., 2009, In : Journal of Pharmacology and Experimental Therapeutics. 328, p. 893 - 899 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Current and emerging trends in cell-based assays

Jordan, R., Bielefield-Sevigny, M., Christopoulos, A., Eglen, R. M., Mark, D. F., Pfleger, K., Valler, M. J. & Zaman, G. J. R., Dec 2009, In : Drug Discovery World. 11, 1, p. 66-78 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Dualsteric GPCR targeting: A novel route to binding and signaling pathway selectivity

Antony, J., Kellershohn, K., Mohr-Andra, M., Kebig, A., Prilla, S., Muth, M., Heller, E., Disingrini, T., Dallanoce, C., Bertoni, S., Schrobang, J., Trankle, C., Kostenis, E., Christopoulos, A., Holtje, H-D., Barocelli, E., De Amici, M., Holzgrabe, U. & Mohr, K., 2009, In : FASEB Journal. 23, p. 442 - 450 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Effect of the calcimimetic R-568 [3-(2-chlorophenyl)-N-((1R)-1-(3- methoxyphenyl)ethyl)-1-propanamine] on correcting inactivating mutations in the human calcium-sensing receptor

Lu, J. Y. L., Yang, Y., Gnacadja, G., Christopoulos, A. & Reagan, J. D., 2009, In : Journal of Pharmacology and Experimental Therapeutics. 331, 3, p. 775 - 786 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Functional importance of a structurally distinct homodimeric complex of the family B G protein-coupled secretin receptor

Gao, F., Harikumar, K. G., Dong, M., Lam, P. C-H., Sexton, P. M., Christopoulos, A., Bordner, A., Abagyan, R. & Miller, L. J., 2009, In : Molecular Pharmacology. 76, 2, p. 264 - 274 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Homology Modeling of GPCRs

Simms, J. W., Hall, N. E., Lam, P. HC., Christopoulos, A., Abagyan, R. & Sexton, P., 2009, Methods in Molecular Biology - G Protein-Coupled Receptors in Drug Delivery. Leifert, W. R. (ed.). 552 ed. USA: Humana Press, p. 97 - 113 17 p.

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

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