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Research Output 1993 2019

2014

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
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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

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 othersRigon, 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

Probing structural requirements of positive allosteric modulators of the M4 muscarinic receptor

Huynh, T., Valant, C., Crosby, I. T., Sexton, P., Christopoulos, A. & Capuano, B., 2013, In : Journal of Medicinal Chemistry. 56, 20, p. 8196 - 8200 5 p.

Research output: Contribution to journalArticleResearchpeer-review

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

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

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

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

Tyrosine sulfation of chemokine receptor CCR2 enhances interactions with both monomeric and dimeric forms of the chemokine monocyte chemoattractant protein-1 (MCP-1)

Tan Hoong Yu, J., Ludeman, J. P., Wedderburn, J., Canals, M., Hall, P. H., Butler, S. J., Taleski, D., Christopoulos, A., Hickey, M. J., Payne, R. J. & Stone, M. J., 2013, In : Journal of Biological Chemistry. 288, 14, p. 10024 - 10034 11 p.

Research output: Contribution to journalArticleResearchpeer-review

2012

Allosteric modulation of endogenous metabolites as an avenue for drug discovery

Wootten, D. L., Savage, E. E., Valant, C., May, L. T., Sloop, K. W., Ficorilli, J., Showalter, A. D., Willard, F. S., Christopoulos, A. & Sexton, P. M., 2012, In : Molecular Pharmacology. 82, 2, p. 281 - 290 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery

Melancon, B. J., Hopkins, C. R., Wood, M. R., Emmitte, K. A., Niswender, C. M., Christopoulos, A., Conn, P. J. & Lindsley, C. W., 2012, In : Journal of Medicinal Chemistry. 55, 4, p. 1445 - 1464 20 p.

Research output: Contribution to journalArticleResearchpeer-review

A Monod-Wyman-Changeux mechanism can explain G protein-coupled receptor (GPCR) allosteric modulation

Canals, M., Lane, J., Wen, A., Scammells, P., Sexton, P. & Christopoulos, A., 2012, In : Journal of Biological Chemistry. 287, 1, p. 650 - 659 10 p.

Research output: Contribution to journalArticleResearchpeer-review

A simple method for quantifying functional selectivity and agonist bias

Kenakin, T., Watson, C., Muniz-Medina, V., Christopoulos, A. & Novick, S., 2012, In : ACS Chemical Neuroscience. 3, 3, p. 193 - 203 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Consequences of splice variation on secretin family G protein-coupled receptor function

Furness, S. G. B., Wootten, D. L., Christopoulos, A. & Sexton, P. M., 2012, In : British Journal of Pharmacology. 166, 1, p. 98 - 109 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File

Design and receptor interactions of obligate dimeric mutant of chemokine monocyte chemoattractant protein-1 (MCP-1)

Tan Hoong Yu, J., Canals, M., Ludeman, J. P., Wedderburn, J., Boston, C., Butler, S. J., Carrick, A. M., Parody, T. R., Taleski, D., Christopoulos, A., Payne, R. J. & Stone, M. J., 2012, In : Journal of Biological Chemistry. 287, 18, p. 14692 - 14702 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Glucagon-like peptide-1 receptor dimerization differentially regulates agonist signaling but does not affect small molecule allostery

Harikumar, K. G., Wootten, D. L., Pinon, D. I., Koole, C. R., Ball, A. M., Furness, S. GB., Graham, B., Dong, M., Christopoulos, A., Miller, L. J. & Sexton, P. M., 2012, In : Proceedings of the National Academy of Sciences. 109, 45, p. 18607 - 18612 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File

Identification of molecular phenotypes and biased signaling induced by naturally occurring mutations of the human calcium-sensing receptor

Leach, K., Wen, C., Davey, A. E., Sexton, P. M., Conigrave, A. D. & Christopoulos, A., 2012, In : Endocrinology. 153, 9, p. 4304 - 4316 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Positive and negative allosteric modulators promote biased signaling at the calcium-sensing receptor

Davey, A. E., Leach, K., Valant, C., Conigrave, A. D., Sexton, P. M. & Christopoulos, A., 2012, In : Endocrinology. 153, 3, p. 1232 - 1241 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Preface

Fryer, A. D., Christopoulos, A. & Nathanson, N. M., 2012, Muscarinic Receptors. Vol. 208. (Handbook of Experimental Pharmacology; vol. 208).

Research output: Chapter in Book/Report/Conference proceedingForeword / PostscriptOtherpeer-review