1993 …2023
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Research Output 1993 2019

2015

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

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

Use of hemi-equilibrium to determine the dissociation kinetics of histamine H3 receptor antagonists.

Bosnyak, S., Riddy, D., Cook, A. E., Diepenhorst, N., Sexton, P. M., Christopoulos, A. & Langmead, C., 2014. 1 p.

Research output: Contribution to conferencePosterOtherpeer-review

2013

Activation and allosteric modulation of a muscarinic acetylcholine receptor

Kruse, A. C., Ring, A. M., Manglik, A., Hu, J., Hu, K., Eitel, K., Hubner, H., Pardon, E., Valant, C., Sexton, P., Christopoulos, A., Felder, C. C., Gmeiner, P., Steyaert, J., Weis, W., Garcia, K. C., Wess, J. & Kobilka, B., 2013, In : Nature. 504, 7478, p. 101 - 106 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Allosteric modulation of a chemogenetically modified G protein-coupled receptor

Abdul Ridha, A., Lane, J. R. D., Sexton, P., Canals, M. & Christopoulos, A., 2013, In : Molecular Pharmacology. 83, 2, p. 521 - 530 10 p.

Research output: Contribution to journalArticleResearchpeer-review

A simple method to generate stable cell lines for the analysis of transient protein-protein interactions

Savage, E. E., Wootten, D. L., Christopoulos, A., Sexton, P. & Furness, S. G. B., 2013, In : BioTechniques. 54, 4, p. 217 - 221 5 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File

A structure-activity analysis of biased agonism at the dopamine D2 receptor

Shonberg, J., Klein Herenbrink, C., Lopez, L., Christopoulos, A., Scammells, P. J., Capuano, B. & Lane, J. R. D., 2013, In : Journal of Medicinal Chemistry. 56, 22, p. 9199 - 9221 23 p.

Research output: Contribution to journalArticleResearchpeer-review

Bridging the gap: bitopic ligands of G-protein-coupled receptors

Lane, J. R. D., Sexton, P. M. & Christopoulos, A., 2013, In : Trends in Pharmacological Sciences. 34, 1, p. 59 - 66 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Calcium-sensing receptor-dependent activation of CREB phosphorylation in HEK293 cells and human parathyroid cells

Avlani, V. A., Ma, W., Mun, H., Leach, K., Delbridge, L., Christopoulos, A. & Conigrave, A., 2013, In : American Journal of Physiology - Endocrinology and Metabolism. 304, 10, p. 1097 - 1104 8 p.

Research output: Contribution to journalArticleResearchpeer-review

CGRP/adrenomedullin

Wootten, D. L., Tilakaratne, N., Christopoulos, A. & Sexton, P., 2013, Handbook of Biologically Active Peptides. Kastin, A. J. (ed.). Second Edition ed. San Diego CA USA: Elsevier, p. 744 - 751 8 p.

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

Development of M1 mAChR allosteric and bitopic ligands: Prospective therapeutics for the treatment of cognitive deficits

Davie, B. J., Christopoulos, A. & Scammells, P. J., 2013, In : ACS Chemical Neuroscience. 4, 7, p. 1026 - 1048 23 p.

Research output: Contribution to journalArticleResearchpeer-review

Differential activation and modulation of the glucagon-like peptide-1 receptor by small molecule ligands

Wootten, D. L., Savage, E. E., Willard, F. S., Bueno, A. B., Sloop, K. W., Christopoulos, A. & Sexton, P., 2013, In : Molecular Pharmacology. 83, 4, p. 822 - 834 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Emerging paradigms in GPCR allostery: implications for drug discovery

Wootten, D. L., Christopoulos, A. & Sexton, P., 2013, In : Nature Reviews Drug Discovery. 12, 8, p. 630 - 644 15 p.

Research output: Contribution to journalArticleResearchpeer-review

Erratum: Differential activation and modulation of the glucagon-like peptide-1 receptor by small molecular ligands (Molecular Pharmacology (2013) 83 (822-834))

Wootten, D., Savage, E. E., Willard, F. S., Bueno, A. B., Sloop, K. W., Christopoulos, A. & Sexton, P. M., Jul 2013, In : Molecular Pharmacology. 84, 1, p. 170 1 p.

Research output: Contribution to journalComment / DebateOtherpeer-review

Impact of chronic congestive heart failure on pharmacokinetics and vasomotor effects of infused nitrite

Maher, A. R., Arif, S., Madhani, M., Abozguia, K., Ahmed, I., Fernandez, B. O., Feelisch, M., O'Sullivan, A. G., Christopoulos, A., Sverdlov, A. L., Ngo, D., Dautov, R., James, P. E., Horowitz, J. D. & Frenneaux, M. P., 2013, In : British Journal of Pharmacology. 169, 3, p. 659 - 670 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Impact of clinically relevant mutations on the pharmacoregulation and signaling bias of the calcium-sensing receptor by positive and negative allosteric modulators

Leach, K., Wen, C., Cook, A. E., Sexton, P., Conigrave, A. & Christopoulos, A., 2013, In : Endocrinology. 154, 3, p. 1105 - 1116 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Inhibition of tumor angiogenesis and growth by a small-molecule multi-FGF receptor blocker with allosteric properties

Bono, F., De Smet, F., Herbert, C., De Bock, K., Georgiadou, M., Fons, P., Tjwa, M., Alcouffe, C., Ny, A., Bianciotto, M., Jonckx, B., Murakami, M., Lanahan, A. A., Michielsen, C., Sibrac, D., Dol-Gleizes, F., Mazzone, M., Zacchigna, S., Herault, J-P., Fischer, C. & 33 others, Rigon, P., Ruiz de Almodovar, C., Claes, F., Blanc, I., Poesen, K., Zhang, Z., Segura, I., Gueguen, G., Bordes, M-F., Lambrechts, D., Broussy, R., van de Wouwer, M., Michaux, C., Shimada, T., Jean, I., Blacher, S., Noel, A., Motte, P., Rom, E., Rakic, J-M., Katsuma, S., Schaeffer, P., Yayon, A., Van Schepdael, A., Schwalbe, H., Gervasio, F. L., Carmeliet, G., Rozensky, J., Dewerchin, M., Simons, M., Christopoulos, A., Herbert, J-M. & Carmeliet, P., 2013, In : Cancer Cell. 23, 4, p. 477 - 488 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Measurements of ligand bias and functional affinity

Kenakin, T. & Christopoulos, A., 2013, In : Nature Reviews Drug Discovery. 12, 6, p. 483 - 483 1 p.

Research output: Contribution to journalLetterOther

Minireview: Signal bias, allosterism, and polymorphic variation at the GLP-1R: implications for drug discovery

Koole, C. R., Savage, E. E., Christopoulos, A., Miller, L. J., Sexton, P. & Wootten, D. L., 2013, In : Molecular Endocrinology. 27, 8, p. 1234 - 1244 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Molecular basis for benzodiazepine agonist action at the type 1 cholecystokinin receptor

Harikumar, K. G., Cawston, E. E., Lam, P. C. H., Patil, A., Orry, A., Henke, B., Abagyan, R., Christopoulos, A., Sexton, P. & Miller, L. J., 2013, In : Journal of Biological Chemistry. 288, 29, p. 21082 - 21095 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Polar transmembrane interactions drive formation of ligand-specific and signal pathway-biased family B G protein-coupled receptor conformations

Wootten, D. L., Simms, J. W., Miller, L. J., Christopoulos, A. & Sexton, P., 2013, In : Proceedings of the National Academy of Sciences. 110, 13, p. 5211 - 5216 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access