If you made any changes in Pure these will be visible here soon.

Research Output 1993 2019

2016

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

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

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