1993 …2023
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Research Output 1993 2019

Ligand-dependent modulation of G protein conformation alters drug efficacy

Furness, S. G. B., Liang, Y-L., Nowell, C. J., Halls, M. L., Wookey, P. J., Dal Maso, E., Inoue, A., Christopoulos, A., Wootten, D. & Sexton, P. M., 20 Oct 2016, In : Cell. 167, 3, p. 739-749 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Ligand-independent adenosine A2B receptor constitutive activity as a promoter of prostate cancer cell proliferation

Vecchio, E. A., Tan, C. Y. R., Gregory, K., Christopoulos, A., White, P. J. & May, L. T., 1 Apr 2016, In : Journal of Pharmacology and Experimental Therapeutics. 357, 1, p. 36-44 9 p.

Research output: Contribution to journalArticleResearchpeer-review

Microglial activation and progressive brain changes in schizophrenia

Laskaris, L., Di Biase, M. A., Everall, I. P., Chana, G., Christopoulos, A., Skafidas, E. S., Cropley, V. L. & Pantelis, C., 2016, In : British Journal of Pharmacology. 173, 4, p. 666-680 15 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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Molecular mechanisms of action of M5 muscarinic acetylcholine receptor allosteric modulators

Berizzi, A. E., Gentry, P. R., Rueda, P., Hoedt, S. D., Sexton, P. M., Langmead, C. J. & Christopoulos, A., 1 Oct 2016, In : Molecular Pharmacology. 90, 4, p. 427-436 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Murine GPRC6A mediates cellular responses to L-amino acids, but not osteocalcin variants

Rueda, P., Harley, E., Lu, Y., Stewart, G. D., Fabb, S., Diepenhorst, N., Cremers, B., Rouillon, M-H., Wehrle, I., Geant, A., Lamarche, G., Leach, K., Charman, W. N., Christopoulos, A., Summers, R. J., Sexton, P. M. & Langmead, C. J., 1 Jan 2016, In : PLoS ONE. 11, 1, p. 1-19 19 p., e0146846.

Research output: Contribution to journalArticleResearchpeer-review

Open Access

Novel fused arylpyrimidinone based allosteric modulators of the M1 muscarinic acetylcholine receptor

Mistry, S. N., Lim, H., Jorg, M., Capuano, B., Christopoulos, A., Lane, J. R. & Scammells, P. J., 18 May 2016, In : ACS Chemical Neuroscience. 7, 5, p. 647-661 15 p.

Research output: Contribution to journalArticleResearchpeer-review

Novel irreversible agonists acting at the A1 adenosine receptor

Jorg, M., Glukhova, A., Abdul Ridha, A., Vecchio, E. A., Nguyen, A., Sexton, P., White, P., May, L., Christopoulos, A. & Scammells, P., 22 Dec 2016, In : Journal of Medicinal Chemistry. 59, 24, p. 11182-11194 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Prediction of loops in G protein-coupled receptor homology models: effect of imprecise surroundings and constraints

Arora, B., Coudrat, T., Wootten, D., Christopoulos, A., Noronha, S. B. & Sexton, P. M., 25 Apr 2016, In : Journal of Chemical Information and Modeling. 56, 4, p. 671-686 16 p.

Research output: Contribution to journalArticleResearchpeer-review

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

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

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

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

Systematic analysis of factors influencing observations of biased agonism at the mu-opioid receptor

Thompson, G. L., Lane, J. R., Coudrat, T., Sexton, P. M., Christopoulos, A. & Canals, M., 1 Aug 2016, In : Biochemical Pharmacology. 113, p. 70-87 18 p.

Research output: Contribution to journalArticleResearchpeer-review

The complexity of signalling mediated by the glucagon-like peptide-1 receptor

Fletcher, M. M., Halls, M. L., Christopoulos, A., Sexton, P. M. & Wootten, D., 15 Apr 2016, In : Biochemical Society Transactions. 44, 2, p. 582-588 7 p.

Research output: Contribution to journalArticleResearchpeer-review

The extracellular surface of the GLP-1 receptor is a molecular trigger for biased agonism

Wootten, D., Reynolds, C. A., Smith, K. J., Mobarec, J. C., Koole, C., Savage, E. E., Pabreja, K., Simms, J., Sridhar, R., Furness, S. G. B., Liu, M., Thompson, P. E., Miller, L. J., Christopoulos, A. & Sexton, P. M., 16 Jun 2016, In : Cell. 165, 7, p. 1632-1643 12 p.

Research output: Contribution to journalArticleResearchpeer-review

The hybrid molecule, VCP746, is a potent adenosine A2B receptor agonist that stimulates anti-fibrotic signalling

Vecchio, L., Chuo, C. H., Baltos, J-A., Ford, L., Scammells, P. J., Wang, B. H., Christopoulos, A., White, P. J. & May, L. T., 1 Oct 2016, In : Biochemical Pharmacology. 117, p. 46-56 11 p.

Research output: Contribution to journalArticleResearchpeer-review

The role of kinetic context in apparent biased agonism at GPCRs

Herenbrink, C. K., Sykes, D. A., Donthamsetti, P., Canals, M., Coudrat, T., Shonberg, J., Scammells, P. J., Capuano, B., Sexton, P. M., Charlton, S. J., Javitch, J. A., Christopoulos, A. & Lane, J. R., 24 Feb 2016, In : Nature Communications. 7, 14 p., 10842.

Research output: Contribution to journalArticleResearchpeer-review

Open Access

Towards a structural understanding of allosteric drugs at the human calcium-sensing receptor

Leach, K., Gregory, K., Kufareva, I., Khajehali, E., Cook, A. E., Abagyan, R., Conigrave, A. D., Sexton, P. M. & Christopoulos, A., 1 May 2016, In : Cell Research. 26, 5, p. 574-592 19 p.

Research output: Contribution to journalArticleResearchpeer-review

Use of cysteine trapping to map spatial approximations between residues contributing to the helix N-capping motif of secretin and distinct residues within each of the extracellular loops of its receptor

Dong, M., Lam, P. C. H., Orry, A., Sexton, P. M., Christopoulos, A., Abagyan, R. & Miller, L. J., 4 Mar 2016, In : Journal of Biological Chemistry. 291, 10, p. 5172-5184 13 p.

Research output: Contribution to journalArticleResearchpeer-review

2017

A kinetic view of GPCR allostery and biased agonism

Lane, J. R., May, L. T., Parton, R. G., Sexton, P. M. & Christopoulos, A., 18 Aug 2017, In : Nature Chemical Biology. 13, 9, p. 929-937 9 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

Open Access
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Allosteric modulation as a unifying mechanism for receptor function and regulation

Changeux, J-P. & Christopoulos, A., 1 Sep 2017, In : Diabetes, Obesity and Metabolism. 19, p. 4-21 18 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

Open Access
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Allostery and Biased Agonism at Class B G Protein-Coupled Receptors

Wootten, D., Miller, L. J., Koole, C., Christopoulos, A. & Sexton, P. M., 11 Jan 2017, In : Chemical Reviews. 117, 1, p. 111-138 28 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: implications for optimizing preclinical neuroscience drug discovery

Sengmany, K., Singh, J., Stewart, G. D., Conn, P. J., Christopoulos, A. & Gregory, K. J., 15 Mar 2017, In : Neuropharmacology. 115, p. 60-72 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Capadenoson, a clinically trialed partial adenosine A1 receptor agonist, can stimulate adenosine A2B receptor biased agonism

Baltos, J-A., Vecchio, E. A., Harris, M. A., Qin, C. X., Ritchie, R. H., Christopoulos, A., White, P. J. & May, L. T., 1 Jul 2017, In : Biochemical Pharmacology. 135, p. 79–89 11 p.

Research output: Contribution to journalArticleResearchpeer-review

High throughput, quantitative analysis of human osteoclast differentiation and activity

Diepenhorst, N., Nowell, C., Rueda, P., Henriksen, K., Pierce, T., Cook, A., Pastoureau, P., Sabatini, M., Charman, W., Christopoulos, A., Summers, R., Sexton, P. & Langmead, C., 15 Feb 2017, In : Analytical Biochemistry. 519, p. 51-56 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Improving virtual screening of G protein-coupled receptors via ligand-directed modeling

Coudrat, T., Simms, J., Christopoulos, A., Wootten, D. & Sexton, P. M., 1 Nov 2017, In : PLoS Computational Biology. 13, 11, 40 p., e1005819.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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Isoform-specific biased agonism of histamine H3 receptor agonists

Riddy, D. M., Cook, A. E., Diepenhorst, N. A., Bosnyak, S., Brady, R., La Cour, C. M., Mocaer, E., Summers, R. J., Charman, W. N., Sexton, P. M., Christopoulos, A. & Langmead, C. J., 1 Feb 2017, In : Molecular Pharmacology. 91, 2, p. 87-99 13 p.

Research output: Contribution to journalArticleResearchpeer-review

M1 muscarinic allosteric modulators slow prion neurodegeneration and restore memory loss

Bradley, S. J., Bourgognon, J. M., Sanger, H. E., Verity, N., Mogg, A. J., White, D. J., Butcher, A. J., Moreno, J. A., Molloy, C., Macedo-Hatch, T., Edwards, J. M., Wess, J., Pawlak, R., Read, D. J., Sexton, P. M., Broad, L. M., Steinert, J. R., Mallucci, G. R., Christopoulos, A., Felder, C. C. & 1 othersTobin, A. B., 1 Feb 2017, In : Journal of Clinical Investigation. 127, 2, p. 487-499 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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Phase-plate cryo-EM structure of a class B GPCR-G-protein complex

Liang, Y-L., Khoshouei, M., Radjainia, M., Zhang, Y., Glukhova, A., Tarrasch, J., Thal, D., Furness, S. G. B., Christopoulos, G., Coudrat, T., Danev, R., Baumeister, W., Miller, L. J., Christopoulos, A., Kobilka, B., Wootten, D., Skiniotis, G. & Sexton, P., 1 Jun 2017, In : Nature. 546, 7656, p. 118-123 6 p.

Research output: Contribution to journalArticleResearchpeer-review

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
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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

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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

THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: Overview

Alexander, S. P. H., Kelly, E., Marrion, N. V., Peters, J. A., Faccenda, E., Harding, S. D., Pawson, A. J., Sharman, J. L., Southan, C., Buneman, O. P., Cidlowski, J. A., Christopoulos, A., Davenport, A. P., Fabbro, D., Spedding, M., Striessnig, J., Davies, J. A. & CGTP Collaborators, 1 Dec 2017, In : British Journal of Pharmacology. 174, S1, p. S1-S16 16 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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Bitopic binding mode of an M1 muscarinic acetylcholine receptor agonist associated with adverse clinical trial outcomes S

Bradley, S. J., Molloy, C., Bundgaard, C., Mogg, A. J., Thompson, K. J., Dwomoh, L., Sanger, H. E., Crabtree, M. D., Brooke, S. M., Sexton, P. M., Felder, C. C., Christopoulos, A., Broad, L. M., Tobin, A. B. & Langmead, C. J., 1 Jun 2018, In : Molecular Pharmacology. 93, 6, p. 645-656 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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Characterization of signalling and regulation of common calcitonin receptor splice variants and polymorphisms

Dal Maso, E., Just, R., Hick, C., Christopoulos, A., Sexton, P. M., Wootten, D. & Furness, S. G. B., 1 Feb 2018, In : Biochemical Pharmacology. 148, p. 111-129 19 p.

Research output: Contribution to journalArticleResearchpeer-review

Cryo-EM structure of the active, Gs-protein complexed, human CGRP receptor

Liang, Y-L., Khoshouei, M., Deganutti, G., Glukhova, A., Koole, C., Peat, T. S., Radjainia, M., Plitzko, J. M., Baumeister, W., Miller, L. J., Hay, D. L., Christopoulos, A., Reynolds, C. A., Wootten, D. & Sexton, P. M., 27 Sep 2018, In : Nature. 561, 7724, p. 492-497 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Discovery and Optimization of Potent and CNS Penetrant M5-Preferring Positive Allosteric Modulators Derived from a Novel, Chiral N-(Indanyl)piperidine Amide Scaffold

Bender, A. M., Cho, H. P., Nance, K. D., Lingenfelter, K. S., Luscombe, V. B., Gentry, P. R., Voigtritter, K., Berizzi, A. E., Sexton, P. M., Langmead, C. J., Christopoulos, A., Locuson, C. W., Bridges, T. M., Chang, S., O'Neill, J. C., Zhan, X., Niswender, C. M., Jones, C. K., Conn, P. J. & Lindsley, C. W., 18 Jul 2018, In : ACS Chemical Neuroscience. 9, 7, p. 1572-1581 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Divergent effects of strontium and calcium-sensing receptor positive allosteric modulators (calcimimetics) on human osteoclast activity

Diepenhorst, N. A., Leach, K., Keller, A. N., Rueda, P., Cook, A. E., Pierce, T. L., Nowell, C., Pastoureau, P., Sabatini, M., Summers, R. J., Charman, W. N., Sexton, P. M., Christopoulos, A. & Langmead, C. J., 1 Nov 2018, In : British Journal of Pharmacology. 175, 21, p. 4095-4108 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Extracellular loops 2 and 3 of the calcitonin receptor selectively modify agonist binding and efficacy

Dal Maso, E., Zhu, Y., Pham, V., Reynolds, C. A., Deganutti, G., Hick, C. A., Yang, D., Christopoulos, A., Hay, D. L., Wang, M. W., Sexton, P. M., Furness, S. G. B. & Wootten, D., 1 Apr 2018, In : Biochemical Pharmacology. 150, p. 214-244 31 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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Glucagon-like peptide-1 receptor internalisation controls spatiotemporal signalling mediated by biased agonists

Fletcher, M. M., Halls, M. L., Zhao, P., Clydesdale, L., Christopoulos, A., Sexton, P. M. & Wootten, D., 1 Oct 2018, In : Biochemical Pharmacology. 156, p. 406-419 14 p.

Research output: Contribution to journalArticleResearchpeer-review