1993 …2023
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Research Output 1993 2020

2010
130 Citations (Scopus)

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

Koole, C., Wootten, D., Simms, J., Valant, C., Sridhar, R., Woodman, O., Miller, L. J., Summers, R., Christopoulos, A. & Sexton, P. M., 2010, In : Molecular Pharmacology. 78, 3, p. 456 - 465 10 p.

Research output: Contribution to journalArticleResearchpeer-review

33 Citations (Scopus)

Delineating the mode of action of adenosine A1 receptor allosteric modulators

Valant, C., Aurelio, L., Urmaliya, V., White, P., Scammells, P., Sexton, P. & Christopoulos, A., 2010, In : Molecular Pharmacology. 78, 3, p. 444 - 455 12 p.

Research output: Contribution to journalArticleResearchpeer-review

21 Citations (Scopus)

Detection of novel functional selectivity at M3 muscarinic acetylcholine receptors using a Saccharomyces cerevisiae platform

Stewart, G. D., Sexton, P. & Christopoulos, A., 2010, In : ACS Chemical Biology. 5, 4, p. 365 - 375 11 p.

Research output: Contribution to journalArticleResearchpeer-review

23 Citations (Scopus)

Effects of conformational restriction of 2-amino-3-benzoylthiophenes on A1 adenosine receptor modulation

Aurelio, L., Valant, C., Flynn, B., Sexton, P., White, J., Christopoulos, A. & Scammells, P., 2010, In : Journal of Medicinal Chemistry. 53, p. 6550 - 6559 10 p.

Research output: Contribution to journalArticleResearchpeer-review

23 Citations (Scopus)

H2 relaxin is a biased ligand relative to H3 relaxin at the relaxin family peptide receptor 3 (RXFP3) [S]

van der Westhuizen, E. T., Christopoulos, A., Sexton, P., Wade, J. & Summers, R., 2010, In : Molecular Pharmacology. 77, 5, p. 759 - 772 14 p.

Research output: Contribution to journalArticleResearchpeer-review

117 Citations (Scopus)

Identification of orthosteric and allosteric site mutations in M 2 muscarinic acetylcholine receptors that contribute to ligand-selective signaling bias

Gregory, K. J., Hall, N., Tobin, A., Sexton, P. & Christopoulos, A., 2010, In : Journal of Biological Chemistry. 285, 10, p. 7459 - 7474 16 p.

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)

Measurement of ligand-G protein-coupled receptor interactions

Leach, K., Valant, C., Sexton, P. M. & Christopoulos, A., 25 Jan 2010, G Protein-Coupled Receptors: Essential Methods. Poyner, D. R. & Wheatley, M. (eds.). Chichester UK: Wiley-Blackwell, p. 1-29 29 p. (Proteins & Macromolecules).

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

115 Citations (Scopus)

Molecular mechanisms of action and in vivo validation of an M4 muscarinic acetylcholine receptor allosteric modulator with potential antipsychotic properties

Leach, K., Loiacono, R. E., Felder, C. C., McKinzie, D. L., Mogg, A., Shaw, D. B., Sexton, P. M. & Christopoulos, A., 2010, In : Neuropsychopharmacology. 35, 4, p. 855 - 869 15 p.

Research output: Contribution to journalArticleResearchpeer-review

51 Citations (Scopus)

Orthosteric and allosteric modes of interaction of novel selective agonists of the M1 muscarinic acetylcholine receptor

Avlani, V. A., Langmead, C. J., Guida, E., Wood, M. D., Tehan, B. G., Herdon, H. J., Watson, J. M., Sexton, P. & Christopoulos, A., 2010, In : Molecular Pharmacology. 78, 1, p. 94 - 104 11 p.

Research output: Contribution to journalArticleResearchpeer-review

27 Citations (Scopus)

Overview of receptor allosterism

Gregory, K., Sexton, P. & Christopoulos, A., Dec 2010, In : Current Protocols in Pharmacology. Chapter 1, Supp 51, p. 1.21-1 - 1.21-34 1 p.

Research output: Contribution to journalArticleResearchpeer-review

17 Citations (Scopus)
7 Citations (Scopus)

Receptor activity modifying proteins and their potential as drug targets

Wootten, D., Simms, J. W., Hay, D. L., Christopoulos, A. & Sexton, P., 2010, Progress in Molecular Biology and Translational Science. Lunn, C. A. (ed.). 1st ed. UK: Academic Press, p. 53 - 79 27 p.

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

1 Citation (Scopus)

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

51 Citations (Scopus)
37 Citations (Scopus)

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

4 Citations (Scopus)

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

1 Citation (Scopus)

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
26 Citations (Scopus)

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

670 Citations (Scopus)

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

88 Citations (Scopus)
32 Citations (Scopus)

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

106 Citations (Scopus)

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

33 Citations (Scopus)

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

40 Citations (Scopus)

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

11 Citations (Scopus)

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

53 Citations (Scopus)

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

69 Citations (Scopus)

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
38 Citations (Scopus)

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

163 Citations (Scopus)

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

129 Citations (Scopus)
16 Citations (Scopus)

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

50 Citations (Scopus)

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

85 Citations (Scopus)

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

14 Citations (Scopus)

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

34 Citations (Scopus)

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

74 Citations (Scopus)

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
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109 Citations (Scopus)

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

14 Citations (Scopus)

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

5 Citations (Scopus)

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

10 Citations (Scopus)

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

9 Citations (Scopus)

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
247 Citations (Scopus)

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

481 Citations (Scopus)

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

75 Citations (Scopus)

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

118 Citations (Scopus)

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

81 Citations (Scopus)

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

780 Citations (Scopus)

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

1 Citation (Scopus)

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