1993 …2023
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Research Output 1993 2020

Article
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

29 Citations (Scopus)

Prolonged calcitonin receptor signaling by salmon, but not human calcitonin, reveals ligand bias

Andreassen, K. V., Hjuler, S. T., Furness, S. G. B., Sexton, P. M., Christopoulos, A., Nosjean, O., Karsdal, M. A. & Henriksen, K., 2014, In : PLoS ONE. 9, 3 (Art. No: e92042), p. 1 - 10 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
7 Citations (Scopus)

Proof of concept study for designed multiple ligands targeting the dopamine D2, serotonin 5-HT2A, and muscarinic M1 acetylcholine receptors

Szabo, M., Lim, H. D., Klein Herenbrink, C., Christopoulos, A., Lane, J. R. D. & Capuano, B., 2015, In : Journal of Medicinal Chemistry. 58, 3, p. 1550 - 1555 6 p.

Research output: Contribution to journalArticleResearchpeer-review

26 Citations (Scopus)

Proposed mode of binding and action of positive allosteric modulators at opioid receptors

Shang, Y., Yeatman, H. R., Provasi, D., Alt, A., Christopoulos, A., Canals, M. & Filizola, M., 20 May 2016, In : ACS Chemical Biology. 11, 5, p. 1220-1229 10 p.

Research output: Contribution to journalArticleResearchpeer-review

28 Citations (Scopus)

Quantification of adenosine A1 receptor biased agonism: Implications for drug discovery

Baltos, J-A., Gregory, K. J., White, P. J., Sexton, P. M., Christopoulos, A. & May, L. T., 1 Jan 2016, In : Biochemical Pharmacology. 99, p. 101-112 12 p.

Research output: Contribution to journalArticleResearchpeer-review

10 Citations (Scopus)

Quantification of allosteric interactions at G protein-coupled receptors using radioligand binding assays

Leach, K., Sexton, P. & Christopoulos, A., 2011, In : Current Protocols in Pharmacology. 1, Supp 52 (Unit 1.22), p. 1 - 41 41 p.

Research output: Contribution to journalArticleResearchpeer-review

49 Citations (Scopus)

Quantification of functional selectivity at the human {alpha}1A-adrenoceptor

Evans, B. A., Broxton, N., Merlin, J., Sato, M., Hutchinson, D. S., Christopoulos, A. & Summers, R. J., 2011, In : Molecular Pharmacology. 79, 2, p. 298 - 307 10 p.

Research output: Contribution to journalArticleResearchpeer-review

107 Citations (Scopus)

Quantification of ligand bias for clinically relevant beta2-adrenergic receptor ligands: Implications for drug taxonomy

van der Westhuizen, E. T., Breton, B., Christopoulos, A. & Bouvier, M., 2014, In : Molecular Pharmacology. 85, 3, p. 492 - 509 18 p.

Research output: Contribution to journalArticleResearchpeer-review

82 Citations (Scopus)

RAMPs: 5 years on, where to now?

Morfis, M., Christopoulos, A. & Sexton, P., 2003, In : Trends in Pharmacological Sciences. 24, 11, p. 596 - 601 6 p.

Research output: Contribution to journalArticleResearchpeer-review

13 Citations (Scopus)
44 Citations (Scopus)

Recent advances in understanding GLP-1R (glucagon-like peptide-1 receptor) function

Koole, C. R., Pabreja, K., Savage, E. E., Wootten, D. L., Furness, S. G. B., Miller, L. J., Christopoulos, A. & Sexton, P., 2013, In : Biochemical Society Transactions. 41, 1, p. 172 - 179 8 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
File
15 Citations (Scopus)

Receptor expression modulates calcium-sensing receptor mediated intracellular Ca2+ mobilization

Brennan, S. C., Mun, H., Leach, K., Kuchel, P. W., Christopoulos, A. & Conigrave, A., 2015, In : Endocrinology. 156, 4, p. 1330 - 1342 13 p.

Research output: Contribution to journalArticleResearchpeer-review

3 Citations (Scopus)

Regulation of acetylcholine binding by ATP at the muscarinic M1 receptor in intact CHO cells

Grant, M. K. O., Christopoulos, A. & El-Fakahany, E. E., 21 Aug 1999, In : Brain Research. 839, 1, p. 94-99 6 p.

Research output: Contribution to journalArticleResearchpeer-review

28 Citations (Scopus)
15 Citations (Scopus)

Regulation of serotonin 5-HT{2C} receptors by chronic ligand exposure

Devlin, M. G., Smith, N. J., Ryan, O. M., Guida, E., Sexton, P. M. & Christopoulos, A., 2004, In : European Journal of Pharmacology. 498, 1-3, p. 59 - 69 11 p.

Research output: Contribution to journalArticleResearchpeer-review

157 Citations (Scopus)

Relative affinity of angiotensin peptides and novel ligands at AT1 and AT2 receptors

Bosnyak, S., Jones, E., Christopoulos, A., Aguilar, M., Thomas, W. & Widdop, R., 2011, In : Clinical Science. 121, 7, p. 297 - 303 7 p.

Research output: Contribution to journalArticleResearchpeer-review

71 Citations (Scopus)

Reversible and specific extracellular antagonism of receptor-histidine kinase signaling

Lyon, G. J., Wright, J. S., Christopoulos, A., Novick, R. P. & Muir, T. W., 2002, In : Journal of Biological Chemistry. 277, 8, p. 6247 - 6253 7 p.

Research output: Contribution to journalArticleResearchpeer-review

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

20 Citations (Scopus)

Role of the second extracellular loop of the adenosine A1 receptor on allosteric modulator binding, signaling, and cooperativity

Nguyen, A. T. N., Vecchio, E. A., Thomas, T., Nguyen, T. D., Aurelio, L., Scammells, P. J., White, P. J., Sexton, P. M., Gregory, K. J., May, L. T. & Christopoulos, A., 1 Dec 2016, In : Molecular Pharmacology. 90, 6, p. 715-725 11 p.

Research output: Contribution to journalArticleResearchpeer-review

9 Citations (Scopus)

Roles of intraloops-2 and -3 and the proximal C-terminus in signalling pathway selection from the human calcium-sensing receptor

Goolam, M. A., Ward, J. H., Avlani, V. A., Leach, K., Christopoulos, A. & Conigrave, A., 2014, In : FEBS Letters. 588, 18, p. 3340 - 3346 7 p.

Research output: Contribution to journalArticleResearchpeer-review

19 Citations (Scopus)

Second extracellular loop of human glucagon-like peptide-1 receptor (GLP-1R) differentially regulates orthosteric but not allosteric agonist binding and function

Koole, C. R., Wootten, D. L., Simms, J., Savage, E. E., Miller, L. J., Christopoulos, A. & Sexton, P. M., 2012, In : Journal of Biological Chemistry. 287, 6, p. 3659 - 3673 15 p.

Research output: Contribution to journalArticleResearchpeer-review

56 Citations (Scopus)

Second extracellular loop of human glucagon-like peptide-1 receptor (GLP-1R) has a critical role in GLP-1 peptide binding and receptor activation

Koole, C. R., Wootten, D. L., Simms, J. W., Miller, L. J., Christopoulos, A. & Sexton, P., 2012, In : Journal of Biological Chemistry. 287, 6, p. 3642 - 3658 17 p.

Research output: Contribution to journalArticleResearchpeer-review

56 Citations (Scopus)
Open Access
421 Citations (Scopus)

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

Kenakin, T. & Christopoulos, A., 2013, In : Nature Reviews Drug Discovery. 12, 3, p. 205 - 216 12 p.

Research output: Contribution to journalArticleResearchpeer-review

30 Citations (Scopus)

Small molecule allosteric modulation of the glucagon-like Peptide-1 receptor enhances the insulinotropic effect of oxyntomodulin

Willard, F. S., Wootten, D. L., Showalter, A. D., Savage, E. E., Ficorilli, J., Farb, T. B., Bokvist, K., Alsina-Fernandez, J., Furness, S. GB., Christopoulos, A., Sexton, P. M. & Sloop, K. W., 2012, In : Molecular Pharmacology. 82, 6, p. 1066 - 1073 8 p.

Research output: Contribution to journalArticleResearchpeer-review

24 Citations (Scopus)

Small-molecule-biased formyl peptide receptor agonist compound 17b protects against myocardial ischaemia-reperfusion injury in mice

Qin, C. X., May, L. T., Li, R., Cao, N., Rosli, S., Deo, M., Alexander, A. E., Horlock, D., Bourke, J. E., Yang, Y. H., Stewart, A. G., Kaye, D. M., Du, X. J., Sexton, P. M., Christopoulos, A., Gao, X. M. & Ritchie, R. H., 7 Feb 2017, In : Nature Communications. 8, 13 p., 14232.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
22 Citations (Scopus)

Stimulus bias provides evidence for conformational constraints in the structure of a G protein-coupled receptor

Gregory, K. J., Sexton, P. M., Tobin, A. B. & Christopoulos, A., 2012, In : Journal of Biological Chemistry. 287, 44, p. 37066 - 37077 12 p.

Research output: Contribution to journalArticleResearchpeer-review

8 Citations (Scopus)

Structural Basis for Binding of Allosteric Drug Leads in the Adenosine A1 Receptor

Miao, Y., Bhattarai, A., Nguyen, A. T. N., Christopoulos, A. & May, L. T., 1 Dec 2018, In : Scientific Reports. 8, 1, 13 p., 16836.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
245 Citations (Scopus)

Structural basis for modulation of a G-protein-coupled receptor by allosteric drugs

Dror, R., Green, H. F., Valant, C., Borhani, D. W., Valcourt, J. R., Pan, A. C., Arlow, D. H., Canals, M., Lane, J. R. D., Rahmani, R. S., Baell, J. B., Sexton, P., Christopoulos, A. & Shaw, D. E., 2013, In : Nature. 503, 7475, p. 295 - 299 5 p.

Research output: Contribution to journalArticleResearchpeer-review

41 Citations (Scopus)

Structural basis of receptor sulfotyrosine recognition by a CC chemokine: the N-terminal region of CCR3 bound to CCL11/eotaxin-1

Millard, C. J., Ludeman, J. P., Canals, M., Bridgford, J. L., Hinds, M. G., Clayton, D. J., Christopoulos, A., Payne, R. J. & Stone, M. J., 2014, In : Structure. 22, 11, p. 1571 - 1581 11 p.

Research output: Contribution to journalArticleResearchpeer-review

51 Citations (Scopus)
1 Citation (Scopus)

Structural features embedded in G protein-coupled receptor co-crystal structures are key to their success in virtual screening

Coudrat, T., Christopoulos, A., Sexton, P. M. & Wootten, D., 1 Apr 2017, In : PLoS ONE. 12, 4, 29 p., e0174719.

Research output: Contribution to journalArticleResearchpeer-review

File
22 Citations (Scopus)

Structure-activity analysis of biased agonism at the human adenosine A3 receptor

Baltos, J-A., Paoletta, S., Nguyen, A. T. N., Gregory, K. J., Tosh, D. K., Christopoulos, A., Jacobson, K. A. & May, L. T., 1 Jul 2016, In : Molecular Pharmacology. 90, 1, p. 12-22 11 p.

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)

Structure-Activity Relationships of Pan-Gαq/11 Coupled Muscarinic Acetylcholine Receptor Positive Allosteric Modulators

Berizzi, A. E., Bender, A. M., Lindsley, C. W., Conn, P. J., Sexton, P. M., Langmead, C. J. & Christopoulos, A., 18 Jul 2018, In : ACS Chemical Neuroscience. 9, 7, p. 1818-1828 11 p.

Research output: Contribution to journalArticleResearchpeer-review

45 Citations (Scopus)

Structure-activity relationships of privileged structures lead to the discovery of novel biased ligands at the dopamine D2 receptor

Szabo, M., Klein Herenbrink, C., Christopoulos, A., Lane, J. R. D. & Capuano, B., 2014, In : Journal of Medicinal Chemistry. 57, 11, p. 4924 - 4939 16 p.

Research output: Contribution to journalArticleResearchpeer-review

6 Citations (Scopus)

Structure-Based Design and Discovery of New M2 Receptor Agonists

Fish, I., Stößel, A., Eitel, K., Valant, C., Albold, S., Huebner, H., Möller, D., Clark, M. J., Sunahara, R. K., Christopoulos, A., Shoichet, B. K. & Gmeiner, P., 22 Nov 2017, In : Journal of Medicinal Chemistry. 60, 22, p. 9239-9250 12 p.

Research output: Contribution to journalArticleResearchpeer-review

13 Citations (Scopus)

Structure-based discovery of selective positive allosteric modulators of antagonists for the M2 muscarinic acetylcholine receptor

Korczynska, M., Clark, M. J., Valant, C., Xu, J., Moo, E. V., Albold, S., Weiss, D. R., Torosyan, H., Huang, W., Kruse, A. C., Lyda, B. R., May, L. T., Baltos, J. A., Sexton, P. M., Kobilka, B. K., Christopoulos, A., Shoichet, B. K. & Sunahara, R. K., 6 Mar 2018, In : Proceedings of the National Academy of Sciences. 115, 10, p. E2419-E2428 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
94 Citations (Scopus)

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

80 Citations (Scopus)

Structure of the adenosine A1 receptor reveals the basis for subtype selectivity

Glukhova, A., Thal, D. M., Nguyen, A. T., Vecchio, L., Jorg, M., Scammells, P. J., May, L. T., Sexton, P. M. & Christopoulos, A., 23 Feb 2017, In : Cell. 168, 5, p. 867-877.e13

Research output: Contribution to journalArticleResearchpeer-review

60 Citations (Scopus)

Structure of the adenosine-bound human adenosine A1 receptor-Gi complex

Draper-Joyce, C. J., Khoshouei, M., Thal, D. M., Liang, Y. L., Nguyen, A. T. N., Furness, S. G. B., Venugopal, H., Baltos, J. A., Plitzko, J. M., Danev, R., Baumeister, W., May, L. T., Wootten, D., Sexton, P. M., Glukhova, A. & Christopoulos, A., 20 Jun 2018, In : Nature. 558, 7711, p. 559-565 7 p.

Research output: Contribution to journalArticleResearchpeer-review

20 Citations (Scopus)

Supra-physiological efficacy at GPCRs: superstition or super agonists?

Langmead, C. J. & Christopoulos, A., 2013, In : British Journal of Pharmacology. 169, 2, p. 353 - 356 4 p.

Research output: Contribution to journalArticleOtherpeer-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

34 Citations (Scopus)

Synthesis and characterization of novel 2-amino-3-benzoylthiophene derivatives as biased allosteric agonists and modulators of the adenosine A1 receptor

Valant, C., Aurelio, L., Devine, S. M., Ashton, T. D., White, J. M., Sexton, P. M., Christopoulos, A. & Scammells, P. J., 2012, In : Journal of Medicinal Chemistry. 55, 5, p. 2367 - 2375 9 p.

Research output: Contribution to journalArticleResearchpeer-review

45 Citations (Scopus)

Synthesis and pharmacological evaluation of dimeric muscarinic acetylcholine receptor agonists

Christopoulos, A., Grant, M. K. O., Ayoubzadeh, N., Kim, O. N., Sauerberg, P., Jeppesen, L. & El-Fakahany, E. E., 29 Aug 2001, In : Journal of Pharmacology and Experimental Therapeutics. 298, 3, p. 1260-1268 9 p.

Research output: Contribution to journalArticleResearchpeer-review