1993 …2023
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Research Output 1993 2019

2014

Advances in G protein-coupled receptor allostery: From function to structure

Christopoulos, A., 2014, In : Molecular Pharmacology. 86, 5, p. 463 - 478 16 p.

Research output: Contribution to journalArticleResearchpeer-review

Allosteric modulation of M1 muscarinic acetylcholine receptor internalization and subcellular trafficking

Yeatman, H. R., Lane, J. R. D., Choy, K. H. C., Lambert, N., Sexton, P., Christopoulos, A. & Canals, M., 2014, In : Journal of Biological Chemistry. 289, 22, p. 15856 - 15866 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Allosteric targeting of receptor tyrosine kinases

De Smet, F., Christopoulos, A. & Carmeliet, P., 2014, In : Nature Biotechnology. 32, 11, p. 1113 - 1120 8 p.

Research output: Contribution to journalArticleResearchpeer-review

A new mechanism of allostery in a G protein-coupled receptor dimer

Lane, J. R. D., Donthamsetti, P., Shonberg, J., Draper-Joyce, C. J., Dentry, S., Michino, M., Shi, L., Lopez Munoz, L., Scammells, P. J., Capuano, B., Sexton, P., Javitch, J. A. & Christopoulos, A., 2014, In : Nature Chemical Biology. 10, 9, p. 745 - 752 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Biased agonism at G protein-coupled receptors: The promise and the challenges - A medicinal chemistry perspective

Shonberg, J., Lopez Munoz, L., Scammells, P. J., Christopoulos, A., Capuano, B. & Lane, J. R. D., 2014, In : Medicinal Research Reviews. 34, 6, p. 1286 - 1330 45 p.

Research output: Contribution to journalArticleResearchpeer-review

Characterization of the novel positive allosteric modulator, LY2119620, at the muscarinic M(2) and M(4) receptors

Croy, C. H., Schober, D. A., Xiao, H., Quets, A., Christopoulos, A. & Felder, C. C., 2014, In : Molecular Pharmacology. 86, 1, p. 106 - 115 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Development of a photoactivatable allosteric ligand for the M1 muscarinic acetylcholine receptor

Davie, B. J., Sexton, P., Capuano, B., Christopoulos, A. & Scammells, P. J., 2014, In : ACS Chemical Neuroscience. 5, 10, p. 902 - 907 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Development of a radioligand, [(3)H]LY2119620, to probe the human M(2) and M(4) muscarinic receptor allosteric binding sites

Schober, D. A., Croy, C. H., Xiao, H., Christopoulos, A. & Felder, C. C., 2014, In : Molecular Pharmacology. 86, 1, p. 116 - 123 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Engendering biased signalling from the calcium-sensing receptor for the pharmacotherapy of diverse disorders

Leach, K., Sexton, P., Christopoulos, A. & Conigrave, A., 2014, In : British Journal of Pharmacology. 171, 5, p. 1142 - 1155 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Erratum: Tyrosine sulfation of chemokine receptor CCR2 enhances interactions with both monomeric and dimeric forms of the chemokine monocyte chemoattractant protein-1 (MCP-1): (Journal of Biological Chemistry (2013) 288 (10024-10034))

Tan, J. H. Y., Ludeman, J. P., Wedderburn, J., Canals, M., Hall, P., Butler, S. J., Taleski, D., Christopoulos, A., Hickey, M. J., Payne, R. J. & Stone, M. J., 2014, In : Journal of Biological Chemistry. 289, 19, p. 13362 1 p.

Research output: Contribution to journalComment / DebateOtherpeer-review

Functional and structural perspectives on allosteric modulation of GPCRs

Langmead, C. J. & Christopoulos, A., 2014, In : Current Opinion in Cell Biology. 27, 1, p. 94 - 101 8 p.

Research output: Contribution to journalArticleResearchpeer-review

International union of basic and clinical pharmacology. XC. Multisite pharmacology: Recommendations for the nomenclature of receptor allosterism and allosteric ligands

Christopoulos, A., Changeux, J-P., Catterall, W. A., Fabbro, D., Burris, T. P., Cidlowski, J. A., Olsen, R. W., Peters, J. A., Neubig, R., Pin, J. P., Sexton, P., Kenakin, T. P., Ehlert, F. J., Spedding, M. & Langmead, C. J., 2014, In : Pharmacological Reviews. 66, 4, p. 918 - 947 30 p.

Research output: Contribution to journalArticleResearchpeer-review

Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor

Abdul Ridha, A., Lane, J. R. D., Mistry, S. N., Lopez Munoz, L., Sexton, P., Scammells, P. J., Christopoulos, A. & Canals, M., 2014, In : Journal of Biological Chemistry. 289, 48, p. 33701 - 33711 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor

Abdul Ridha, A., Lopez, L., Keov, P., Thal, D., Mistry, S. N., Sexton, P., Lane, J. R. D., Canals, M. & Christopoulos, A., 2014, In : Journal of Biological Chemistry. 289, 9, p. 6067 - 6079 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Molecular mechanisms of bitopic ligand engagement with the M1 muscarinic acetylcholine receptor

Keov, P., Lopez, L., Devine, S., Valant, C., Lane, J. R. D., Scammells, P. J., Sexton, P. & Christopoulos, A., 2014, In : Journal of Biological Chemistry. 289, 34, p. 23817 - 23837 21 p.

Research output: Contribution to journalArticleResearchpeer-review

Muscarinic acetylcholine receptors: Novel opportunities for drug development

Kruse, A. C., Kobilka, B., Gautam, D., Sexton, P. M., Christopoulos, A. & Wess, J., 2014, In : Nature Reviews Drug Discovery. 13, 7, p. 549 - 560 12 p.

Research output: Contribution to journalArticleResearchpeer-review

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

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

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

Open Access

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

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

2015

Allosteric modulation of chemokine receptors

Tschammer, N., Christopoulos, A. & Kenakin, T., 2015, Chemokines: Chemokines and Their Receptors in Drug Discovery. Tschammer, N. (ed.). Cham Switzerland: Springer, p. 87-117 31 p.

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

A positive allosteric modulator of the adenosine A1 receptor selectively inhibits primary afferent synaptic transmission in a neuropathic pain model

Imlach, W. L., Bhola, R. F., May, L. T., Christopoulos, A. & Christie, M. J., 2015, In : Molecular Pharmacology. 88, 3, p. 460-468 9 p.

Research output: Contribution to journalArticleResearchpeer-review

A structure-activity relationship study of the positive allosteric modulator LY2033298 at the M4 muscarinic acetylcholine receptor

Szabo, M., Huynh, T., Valant, C., Lane, J. R., Sexton, P. M., Christopoulos, A. & Capuano, B., 2015, In : MedChemComm. 6, 11, p. 1998-2003 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Biased agonism and biased allosteric modulation at the CB1 cannabinoid receptors

Khajehali, E., Malone, D. T., Glass, M., Sexton, P., Christopoulos, A. & Leach, K., 2015, In : Molecular Pharmacology. 88, 2, p. 368-379 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Biased agonism of endogenous opioid peptides at the μ-opioid receptor

Thompson, G. L., Lane, J. R. D., Coudrat, T., Sexton, P., Christopoulos, A. & Canals, M., 2015, In : Molecular Pharmacology. 88, 2, p. 335-346 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Biased allosteric modulation at the CaS receptor engendered by structurally diverse calcimimetics

Cook, A. E., Mistry, S. N., Gregory, K. J., Furness, S. G. B., Sexton, P., Scammells, P. J., Conigrave, A., Christopoulos, A. & Leach, K., 2015, In : British Journal of Pharmacology. 172, 1, p. 185 - 200 16 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File

Development of a highly selective allosteric antagonist radioligand for the type 1 cholecystokinin receptor and elucidation of its molecular basis of binding

Dong, M., Vattelana, A. M., Lam, P. C. H., Orry, A., Abagyan, R., Christopoulos, A., Sexton, P., Haines, D. R. & Miller, L. J., 2015, In : Molecular Pharmacology. 87, 1, p. 130-140 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of the δ-opioid receptor

Burford, N. T., Livingston, K. E., Canals, M., Ryan, M. R., Budenholzer, L. M. L., Han, Y., Shang, Y., Herbst, J. J., O'Connell, J., Banks, M., Zhang, L., Filizola, M., Bassoni, D. L., Wehrman, T. S., Christopoulos, A., Traynor, J. R., Gerritz, S. W. & Alt, A., 2015, In : Journal of Medicinal Chemistry. 58, 10, p. 4220-4229 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Discovery of a novel class of negative allosteric modulator of the dopamine D2 receptor through fragmentation of a bitopic ligand

Mistry, S. N., Shonberg, J., Draper-Joyce, C. J., Klein Herenbrink, C., Michino, M., Shi, L., Christopoulos, A., Capuano, B., Scammells, P. J. & Lane, J. R. D., 2015, In : Journal of Medicinal Chemistry. 58, 17, p. 6819-6843 25 p.

Research output: Contribution to journalArticleResearchpeer-review

Endogenous allosteric modulators of G protein-coupled receptors

Van Der Westhuizen, E. T., Valant, C., Sexton, P. & Christopoulos, A., 2015, In : Journal of Pharmacology and Experimental Therapeutics. 353, 2, p. 246 - 260 15 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File

Molecular mechanism of action of triazolobenzodiazepinone agonists of the type 1 cholecystokinin receptor. Possible cooperativity across the receptor homodimeric complex

Desai, A. J., Lam, P. C. H., Orry, A., Abagyan, R., Christopoulos, A., Sexton, P. & Miller, L. J., 2015, In : Journal of Medicinal Chemistry. 58, 24, p. 9562-9577 16 p.

Research output: Contribution to journalArticleResearchpeer-review

Novel allosteric modulators of G protein-coupled receptors

Gentry, P. R., Sexton, P. M. & Christopoulos, A., 2015, In : Journal of Biological Chemistry. 290, 32, p. 19478-19488 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Novel GPCR paradigms at the μ-opioid receptor

Thompson, G. L., Kelly, E., Christopoulos, A. & Canals, M., 2015, In : British Journal of Pharmacology. 172, 2, p. 287-296 10 p.

Research output: Contribution to journalArticleResearchpeer-review

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

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

Synthesis and pharmacological evaluation of M4 muscarinic receptor positive allosteric modulators derived from VU10004

Huynh, T., Valant, C., Crosby, I. T., Sexton, P., Christopoulos, A. & Capuano, B., 2015, In : ACS Chemical Neuroscience. 6, 6, p. 838 - 844 7 p.

Research output: Contribution to journalArticleResearchpeer-review

Towards tissue-specific pharmacology: insights from the calcium-sensing receptor as a paradigm for GPCR (patho)physiological bias

Leach, K., Conigrave, A. D., Sexton, P. M. & Christopoulos, A., 2015, In : Trends in Pharmacological Sciences. 36, 4, p. 215-225 11 p.

Research output: Contribution to journalArticleResearchpeer-review

2016

4-phenylpyridin-2-one derivatives: a novel class of positive allosteric modulator of the M1 muscarinic acetylcholine receptor

Mistry, S. N., Jorg, M., Lim, H., Vinh, N. B., Sexton, P. M., Capuano, B., Christopoulos, A., Lane, J. R. & Scammells, P. J., 14 Jan 2016, In : Journal of Medicinal Chemistry. 59, 1, p. 388-409 22 p.

Research output: Contribution to journalArticleResearchpeer-review

Accelerated structure-based design of chemically diverse allosteric modulators of a muscarinic G protein-coupled receptor

Miao, Y., Goldfeld, D. A., Moo, E. V., Sexton, P. M., Christopoulos, A., McCammon, J. A. & Valant, C., 20 Sep 2016, In : Proceedings of the National Academy of Sciences. 113, 38, p. E5675-E5684 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access

A hydrogen-bonded polar network in the core of the glucagon-like peptide-1 receptor is a fulcrum for biased agonism: lessons from class B crystal structuress

Wootten, D., Reynolds, C. A., Koole, C., Smith, K. J., Mobarec, J. C., Simms, J., Quon, T., Coudrat, T., Furness, S. G. B., Miller, L. J., Christopoulos, A. & Sexton, P. M., 1 Mar 2016, In : Molecular Pharmacology. 89, 3, p. 335-347 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Allosteric Modulation as a Unifying Mechanism for Receptor Function and Regulation

Changeux, J. P. & Christopoulos, A., 25 Aug 2016, In : Cell. 166, 5, p. 1084-1102 19 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 5 Based on Select Acetylenic Negative Allosteric Modulators

Gregory, K., Velagaleti, R., Thal, D. M., Brady, R. M., Christopoulos, A., Conn, P. J. & Lapinsky, D. J., 15 Jul 2016, In : ACS Chemical Biology. 11, 7, p. 1870-1879 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Crystal structures of the M1 and M4 muscarinic acetylcholine receptors

Thal, D. M., Sun, B., Feng, D., Nawaratne, V., Leach, K., Felder, C. C., Bures, M. G., Evans, D. A., Weis, W. I., Bachhawat, P., Kobilka, T. S., Sexton, P. M., Kobilka, B. K. & Christopoulos, A., 17 Mar 2016, In : Nature. 531, 7594, p. 335-340 6 p.

Research output: Contribution to journalArticleResearchpeer-review