1993 …2023
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Research Output 1993 2019

2018

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

Identification of global and ligand-specific calcium sensing receptor activation mechanisms S

Keller, A., Kufareva, I., Josephs, T. M., Diao, J., Mai, V. T-V., Conigrave, A. D., Christopoulos, A., Gregory, K. J. & Leach, K., 1 Jun 2018, In : Molecular Pharmacology. 93, 6, p. 619-630 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Mechanisms of signalling and biased agonism in G protein-coupled receptors

Wootten, D. L., Christopoulos, A., Marti-Solano, M., Babu, M. M. & Sexton, P. M., Oct 2018, In : Nature Reviews Molecular Cell Biology. 19, 10, p. 638-653 16 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

Open Access
File

Muscarinic M5 receptors modulate ethanol seeking in rats

Berizzi, A. E., Perry, C. J., Shackleford, D. M., Lindsley, C. W., Jones, C. K., Chen, N. A., Sexton, P. M., Christopoulos, A., Langmead, C. J. & Lawrence, A. J., 1 Jun 2018, In : Neuropsychopharmacology. 43, 7, p. 1510-1517 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File

New paradigms in adenosine receptor pharmacology: allostery, oligomerization and biased agonism

Vecchio, E. A., Baltos, J. A., Nguyen, A. T. N., Christopoulos, A., White, P. J. & May, L. T., 1 Nov 2018, In : British Journal of Pharmacology. 175, 21, p. 4036-4046 11 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

Phase-plate cryo-EM structure of a biased agonistbound human GLP-1 receptor-Gs complex

Liang, Y. L., Khoshouei, M., Glukhova, A., Furness, S. G. B., Zhao, P., Clydesdale, L., Koole, C., Truong, T. T., Thal, D. M., Lei, S., Radjainia, M., Danev, R., Baumeister, W., Wang, M. W., Miller, L. J., Christopoulos, A., Sexton, P. M. & Wootten, D., 1 Mar 2018, In : Nature. 555, 7694, p. 121-125 5 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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Probing the binding site of novel selective positive allosteric modulators at the M1 muscarinic acetylcholine receptor

Khajehali, E., Valant, C., Jörg, M., Tobin, A. B., Conn, P. J., Lindsley, C. W., Sexton, P. M., Scammells, P. J. & Christopoulos, A., 1 Aug 2018, In : Biochemical Pharmacology. 154, p. 243-254 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File

Rules of Engagement: GPCRs and G Proteins

Glukhova, A., Draper-Joyce, C. J., Sunahara, R. K., Christopoulos, A., Wootten, D. L. & Sexton, P. M., 7 Sep 2018, In : ACS Pharmacology and Translational Sciences. 1, 2, p. 73-83 11 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

Structural Basis for Binding of Allosteric Drug Leads in the Adenosine A1 Receptor

Miao, Y., Bhattarai, A., Nguyen, A. T. N., Christopoulos, A. & May, L. T., 1 Dec 2018, In : Scientific Reports. 8, 1, 13 p., 16836.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File

Structural insights into G-protein-coupled receptor allostery

Thal, D. M., Glukhova, A., Sexton, P. M. & Christopoulos, A., 5 Jul 2018, In : Nature. 559, 7712, p. 45-53 9 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

Structure-Activity Relationships of Pan-Gαq/11 Coupled Muscarinic Acetylcholine Receptor Positive Allosteric Modulators

Berizzi, A. E., Bender, A. M., Lindsley, C. W., Conn, P. J., Sexton, P. M., Langmead, C. J. & Christopoulos, A., 18 Jul 2018, In : ACS Chemical Neuroscience. 9, 7, p. 1818-1828 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Structure-based discovery of selective positive allosteric modulators of antagonists for the M2 muscarinic acetylcholine receptor

Korczynska, M., Clark, M. J., Valant, C., Xu, J., Moo, E. V., Albold, S., Weiss, D. R., Torosyan, H., Huang, W., Kruse, A. C., Lyda, B. R., May, L. T., Baltos, J. A., Sexton, P. M., Kobilka, B. K., Christopoulos, A., Shoichet, B. K. & Sunahara, R. K., 6 Mar 2018, In : Proceedings of the National Academy of Sciences. 115, 10, p. E2419-E2428 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File

Structure of the adenosine-bound human adenosine A1 receptor-Gi complex

Draper-Joyce, C. J., Khoshouei, M., Thal, D. M., Liang, Y. L., Nguyen, A. T. N., Furness, S. G. B., Venugopal, H., Baltos, J. A., Plitzko, J. M., Danev, R., Baumeister, W., May, L. T., Wootten, D., Sexton, P. M., Glukhova, A. & Christopoulos, A., 20 Jun 2018, In : Nature. 558, 7711, p. 559-565 7 p.

Research output: Contribution to journalArticleResearchpeer-review

The action of a negative allosteric modulator at the dopamine D2 receptor is dependent upon sodium ions

Draper-Joyce, C. J., Verma, R. K., Michino, M., Shonberg, J., Kopinathan, A., Klein Herenbrink, C., Scammells, P. J., Capuano, B., Abramyan, A. M., Thal, D. M., Javitch, J. A., Christopoulos, A., Shi, L. & Lane, J. R., 1 Dec 2018, In : Scientific Reports. 8, 1, 12 p., 1208.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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The structural determinants of the bitopic binding mode of a negative allosteric modulator of the dopamine D2 receptor

Draper-Joyce, C. J., Michino, M., Verma, R. K., Klein Herenbrink, C., Shonberg, J., Kopinathan, A., Scammells, P. J., Capuano, B., Thal, D. M., Javitch, J. A., Christopoulos, A., Shi, L. & Lane, J. R., 1 Feb 2018, In : Biochemical Pharmacology. 148, p. 315-328 14 p.

Research output: Contribution to journalArticleResearchpeer-review

To Bind or Not to Bind: Unravelling GPCR Polypharmacology

Sexton, P. M. & Christopoulos, A., 8 Feb 2018, In : Cell. 172, 4, p. 636-638 3 p.

Research output: Contribution to journalShort SurveyOtherpeer-review

Open Access
File

Toward an understanding of the structural basis of allostery in muscarinic acetylcholine receptors

Burger, W. A. C., Sexton, P. M., Christopoulos, A. & Thal, D. M., 1 Oct 2018, In : Journal of General Physiology. 150, 10, p. 1360-1372 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Two distinct domains of the glucagon-like peptide-1 receptor control peptide-mediated biased agonism

Lei, S., Clydesdale, L., Dai, A., Cai, X., Yang, F., Yang, D., Liang, Y-L., Koole, C., Zhao, P., Coudrat, T., Christopoulos, A., Wang, M-W., Wootten, D. & Sexton, P. M., 1 Jan 2018, In : Journal of Biological Chemistry. 293, 24, p. 9370-9387 18 p.

Research output: Contribution to journalArticleResearchpeer-review

2019

6-Phenylpyrimidin-4-ones as Positive Allosteric Modulators at the M1 mAChR: The Determinants of Allosteric Activity

Jorg, M. T., van der Westhuizen, E. T., Khajehali, E., Burger, W. A. C., White, J., Choy, K. H. C., Tobin, A. B., Sexton, P. M., Valant, C., Capuano, B., Christopoulos, A. & Scammells, P. J., 20 Mar 2019, In : ACS Chemical Neuroscience. 10, 3, p. 1099-1114 16 p.

Research output: Contribution to journalArticleResearchpeer-review

Drug-receptor kinetics and sigma-1 receptor affinity differentiate clinically evaluated histamine H3 receptor antagonists

Riddy, D. M., Cook, A. E., Shackleford, D. M., Pierce, T. L., Mocaer, E., Mannoury la Cour, C., Sors, A., Charman, W. N., Summers, R. J., Sexton, P. M., Christopoulos, A. & Langmead, C. J., 1 Jan 2019, In : Neuropharmacology. 144, p. 244-255 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File

Kinetic and system bias as drivers of metabotropic glutamate receptor 5 allosteric modulator pharmacology

Sengmany, K., Hellyer, S. D., Albold, S., Wang, T., Conn, P. J., May, L. T., Christopoulos, A., Leach, K. & Gregory, K. J., 1 May 2019, In : Neuropharmacology. 149, p. 83-96 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Molecular Basis of Action of a Small-Molecule Positive Allosteric Modulator Agonist at the Type 1 Cholecystokinin Holoreceptor

Desai, A. J., Mechin, I., Nagarajan, K., Valant, C., Wootten, D., Lam, P. C. H., Orry, A., Abagyan, R., Nair, A., Sexton, P. M., Christopoulos, A. & Miller, L. J., 1 Mar 2019, In : Molecular Pharmacology. 95, 3, p. 245-259 15 p.

Research output: Contribution to journalArticleResearchpeer-review

The Molecular Control of Calcitonin Receptor Signaling

dal Maso, E., Glukhova, A., Zhu, Y., Garcia-Nafria, J., Tate, C. G., Atanasio, S., Reynolds, C. A., Ramirez-Aportela, E., Carazo, J-M., Hick, C. A., Furness, S. G. B., Hay, D. L., Liang, Y-L., Miller, L. J., Christopoulos, A., Wang, M-W., Wootten, D. & Sexton, P. M., 11 Jan 2019, In : ACS Pharmacology and Translational Sciences. 2, 1, p. 31-51 21 p.

Research output: Contribution to journalArticleResearchpeer-review