1986 …2023

Research output per year

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Article
2016

An allosteric role for receptor activity-modifying proteins in defining GPCR pharmacology

Gingell, J. J., Simms, J., Barwell, J., Poyner, D., Watkins, H. A., Pioszak, A. A., Sexton, P. M. & Hay, D., 17 May 2016, In : Cell Discovery. 2, 14 p., 16012.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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24 Citations (Scopus)

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

136 Citations (Scopus)

Extracellular loop 2 of the adenosine A1 receptor has a key role in orthosteric ligand affinity and agonist efficacy

Nguyen, A. T. N., Baltos, J-A., Thomas, T., Nguyen, T. D., Lopez Munoz, L., Gregory, K. J., White, P. J., Sexton, P. M., Christopoulos, A. & May, L. T., 1 Dec 2016, In : Molecular Pharmacology. 90, 6, p. 703-714 12 p.

Research output: Contribution to journalArticleResearchpeer-review

27 Citations (Scopus)

Glucagon-like peptide-1 and its class B G protein-coupled receptors: a long march to therapeutic successes

de Graaf, C., Donnelly, D., Wootten, D., Lau, J., Sexton, P. M., Miller, L. J., Ahn, J-M., Liao, J., Fletcher, M. M., Yang, D., Brown, A. J. H., Zhou, C., Deng, J. & Wang, M-W., 1 Oct 2016, In : Pharmacological Reviews. 68, 4, p. 954-1013 60 p.

Research output: Contribution to journalArticleResearchpeer-review

65 Citations (Scopus)
19 Citations (Scopus)

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

51 Citations (Scopus)

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

10 Citations (Scopus)

Monotreme glucagon-like peptide-1 in venom and gut: one gene - two very different functions

Tsend-Ayush, E., He, C., Myers, M. A., Andrikopoulos, S., Wong, N., Sexton, P. M., Wootten, D., Forbes, B. E. & Grutzner, F., 29 Nov 2016, In : Scientific Reports. 6, 12 p., 37744.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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5 Citations (Scopus)

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
22 Citations (Scopus)

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

8 Citations (Scopus)
9 Citations (Scopus)

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

5 Citations (Scopus)

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

29 Citations (Scopus)

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

21 Citations (Scopus)

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

31 Citations (Scopus)

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

5 Citations (Scopus)

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

54 Citations (Scopus)

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
126 Citations (Scopus)

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

34 Citations (Scopus)

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

5 Citations (Scopus)

β-arrestin-biased agonists of the GLP-1 receptor from β-amino acid residue incorporation into GLP-1 analogues

Hager, M. V., Johnson, L. M., Wootten, D., Sexton, P. M. & Gellman, S. H., 16 Nov 2016, In : Journal of the American Chemical Society. 138, 45, p. 14970-14979 10 p.

Research output: Contribution to journalArticleResearchpeer-review

23 Citations (Scopus)
2015

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

5 Citations (Scopus)

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

69 Citations (Scopus)

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

44 Citations (Scopus)

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
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41 Citations (Scopus)
Open Access
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6 Citations (Scopus)

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

7 Citations (Scopus)
Open Access
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10 Citations (Scopus)

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
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63 Citations (Scopus)

GPCR structure, function, drug discovery and crystallography: report from Academia-Industry International Conference (UK Royal Society) Chicheley Hall, 1-2 September 2014

Heifetz, A., Schertler, G. F. X., Seifert, R., Tate, C. G., Sexton, P. M., Gurevich, V. V., Fourmy, D., Cherezov, V., Marshall, F., Storer, R. I., Moraes, I., Tikhonova, I., Tautermann, C., Hunt, P., Ceska, T., Hodgson, S., Bodkin, M., Singh, S., Law, R. & Biggin, P., 22 Aug 2015, In : Naunyn-Schmiedeberg's Archives of Pharmacology. 388, 8, p. 883-903 21 p., 1111.

Research output: Contribution to journalArticleOther

Open Access
24 Citations (Scopus)

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

10 Citations (Scopus)

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

90 Citations (Scopus)

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

8 Citations (Scopus)

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

31 Citations (Scopus)
2014

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

18 Citations (Scopus)

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

80 Citations (Scopus)

A nuclear transport inhibitor that modulates the unfolded protein response and provides in vivo protection against lethal dengue virus infection

Fraser, J. E., Watanabe, S., Wang, C., Chan, W. K. K., Maher, B., Lopez-Denman, A., Hick, C. A., Wagstaff, K. M., Mackenzie, J. M., Sexton, P. M., Vasudevan, S. G. & Jans, D. A., 2014, In : Journal of Infectious Diseases. 210, 11, p. 1780 - 1791 12 p.

Research output: Contribution to journalArticleResearchpeer-review

49 Citations (Scopus)

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

8 Citations (Scopus)

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

27 Citations (Scopus)

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

116 Citations (Scopus)

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

32 Citations (Scopus)

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

39 Citations (Scopus)

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

33 Citations (Scopus)

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

172 Citations (Scopus)

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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30 Citations (Scopus)
Open Access
58 Citations (Scopus)

Structural and functional insights into the juxtamembranous amino-terminal tail and extracellular loop regions of class B GPCRs

Dong, M., Koole, C. R., Wootten, D. L., Sexton, P. & Miller, L. J., 2014, In : British Journal of Pharmacology. 171, 5, p. 1085 - 1101 17 p.

Research output: Contribution to journalArticleResearchpeer-review

18 Citations (Scopus)
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

501 Citations (Scopus)