1993 …2020

Research output per year

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Research Output

2020

Acetylcholine Muscarinic M4 Receptors as a Therapeutic Target for Alcohol Use Disorder: Converging Evidence From Humans and Rodents

Walker, L. C., Berizzi, A. E., Chen, N. A., Rueda, P., Perreau, V. M., Huckstep, K., Srisontiyakul, J., Govitrapong, P., Xiaojian, J., Lindsley, C. W., Jones, C. K., Riddy, D. M., Christopoulos, A., Langmead, C. J. & Lawrence, A. J., 28 Feb 2020, (Accepted/In press) In : Biological Psychiatry. 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Activation of the GLP-1 receptor by a non-peptidic agonist

Zhao, P., Liang, Y. L., Belousoff, M. J., Deganutti, G., Fletcher, M. M., Willard, F. S., Bell, M. G., Christe, M. E., Sloop, K. W., Inoue, A., Truong, T. T., Clydesdale, L., Furness, S. G. B., Christopoulos, A., Wang, M. W., Miller, L. J., Reynolds, C. A., Danev, R., Sexton, P. M. & Wootten, D., 8 Jan 2020, In : Nature. 577, 7790, p. 432-436 5 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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5 Citations (Scopus)

Biased M1-muscarinic-receptor-mutant mice inform the design of next-generation drugs

Bradley, S. J., Molloy, C., Valuskova, P., Dwomoh, L., Scarpa, M., Rossi, M., Finlayson, L., Svensson, K. A., Chernet, E., Barth, V. N., Gherbi, K., Sykes, D. A., Wilson, C. A., Mistry, R., Sexton, P. M., Christopoulos, A., Mogg, A. J., Rosethorne, E. M., Sakata, S., John Challiss, R. A. & 2 others, Broad, L. M. & Tobin, A. B., 20 Feb 2020, In : Nature Chemical Biology. 16, 3, p. 240-249 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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1 Citation (Scopus)

Differential contribution of metabotropic glutamate receptor 5 common allosteric binding site residues to biased allosteric agonism

Sengmany, K., Hellyer, S. D., Christopoulos, A., Lapinsky, D. J., Leach, K. & Gregory, K. J., 5 May 2020, (Accepted/In press) In : Biochemical Pharmacology. 15 p., 114011.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

Evaluation of Operational Models of Agonism and Allosterism at Receptors with Multiple Orthosteric Binding Sites

Gregory, K., Giraldo, J., Diao, J., Christopoulos, A. & Leach, K., 2020, In : Molecular Pharmacology. 97, 1, p. 35-45 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
2 Citations (Scopus)

Mu and Delta Opioid Receptors Are Coexpressed and Functionally Interact in the Enteric Nervous System of the Mouse Colon

DiCello, J. J., Carbone, S. E., Saito, A., Rajasekhar, P., Ceredig, R. A., Pham, V., Valant, C., Christopoulos, A., Veldhuis, N. A., Canals, M., Massotte, D. & Poole, D. P., Mar 2020, In : Cellular and Molecular Gastroenterology and Hepatology. 9, 3, p. 465-483 19 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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1 Citation (Scopus)

Toward a Structural Understanding of Class B GPCR Peptide Binding and Activation

Liang, Y. L., Belousoff, M. J., Zhao, P., Koole, C., Fletcher, M. M., Truong, T. T., Julita, V., Christopoulos, G., Xu, H. E., Zhang, Y., Khoshouei, M., Christopoulos, A., Danev, R., Sexton, P. M. & Wootten, D., 6 Feb 2020, In : Molecular Cell. 77, 3, p. 656-668.e5 18 p.

Research output: Contribution to journalArticleResearchpeer-review

3 Citations (Scopus)
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

Open Access
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Cryptic pocket formation underlies allosteric modulator selectivity at muscarinic GPCRs

Hollingsworth, S. A., Kelly, B., Valant, C., Michaelis, J. A., Mastromihalis, O., Thompson, G., Venkatakrishnan, A. J., Hertig, S., Scammells, P. J., Sexton, P. M., Felder, C. C., Christopoulos, A. & Dror, R. O., 1 Dec 2019, In : Nature Communications. 10, 1, p. 1-9 9 p., 3289.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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5 Citations (Scopus)

Crystal structure of the M5 muscarinic acetylcholine receptor

Vuckovic, Z., Gentry, P. R., Berizzi, A. E., Hirata, K., Varghese, S., Thompson, G., van der Westhuizen, E. T., Burger, W. A. C., Rahmani, R., Valant, C., Langmead, C. J., Lindsley, C. W., Baell, J. B., Tobin, A. B., Sexton, P. M., Christopoulos, A. & Thal, D. M., 17 Dec 2019, In : Proceedings of the National Academy of Sciences of the United States of America. 116, 51, p. 26001-26007 7 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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1 Citation (Scopus)

Deconvoluting the Molecular Control of Binding and Signaling at the Amylin 3 Receptor: RAMP3 Alters Signal Propagation through Extracellular Loops of the Calcitonin Receptor

Pham, V., Zhu, Y., Dal Maso, E., Reynolds, C. A., Deganutti, G., Atanasio, S., Hick, C. A., Yang, D., Christopoulos, A., Hay, D. L., Furness, S. G. B., Wang, M-W., Wootten, D. & Sexton, P. M., 18 Mar 2019, In : ACS Pharmacology & Translational Science. 2, 3, p. 183-197 15 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
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6 Citations (Scopus)

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

5 Citations (Scopus)

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

Molecular Determinants of the Intrinsic Efficacy of the Antipsychotic Aripiprazole

Klein Herenbrink, C., Verma, R., Lim, H. D., Kopinathan, A., Keen, A., Shonberg, J., Draper-Joyce, C. J., Scammells, P. J., Christopoulos, A., Javitch, J. A., Capuano, B., Shi, L. & Lane, J. R., 16 Aug 2019, In : ACS Chemical Biology. 14, 8, p. 1780-1792 13 p.

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)

The concise guide to Pharmacology 2019/20: G protein-coupled receptors

Alexander, S. P. H., Christopoulos, A., Davenport, A. P., Kelly, E., Mathie, A., Peters, J. A., Veale, E. L., Armstrong, J. F., Faccenda, E., Harding, S. D., Pawson, A. J., Sharman, J. L., Southan, C., Davies, J. A. & CGTP Collaborators, 1 Dec 2019, In : British Journal of Pharmacology. 176, S1, p. S21-S141 120 p.

Research output: Contribution to journalArticleOtherpeer-review

Open Access
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95 Citations (Scopus)

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 & Translational Science. 2, 1, p. 31-51 21 p.

Research output: Contribution to journalArticleResearchpeer-review

2018
4 Citations (Scopus)

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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9 Citations (Scopus)

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

5 Citations (Scopus)
1 Citation (Scopus)

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

52 Citations (Scopus)
4 Citations (Scopus)

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

2 Citations (Scopus)

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

6 Citations (Scopus)

Dominant Negative G Proteins Enhance Formation and Purification of Agonist-GPCR-G Protein Complexes for Structure Determination

Liang, Y-L., Zhao, P., Draper-Joyce, C. J., Baltos, J-A., Glukhova, A., Truong, T. T., May, L. T., Christopoulos, A., Wootten, D., Sexton, P. & Furness, S., 2018, In : ACS Pharmacology & Translational Science. 1, 1, p. 12-20 9 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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Dual Action Calcium-Sensing Receptor Modulator Unmasks Novel Mode-Switching Mechanism

Gregory, K., Kufareva, I., Keller, A. N., Khajehali, E., Mun, H., Goolam, M. A., Mason, R. S., Capuano, B., Conigrave, A., Christopoulos, A. & Leach, K., 12 Sep 2018, In : ACS Pharmacology & Translational Science. 1, 2, p. 96-109 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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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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11 Citations (Scopus)

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

8 Citations (Scopus)

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

5 Citations (Scopus)

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
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79 Citations (Scopus)

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
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12 Citations (Scopus)

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

15 Citations (Scopus)

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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103 Citations (Scopus)

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
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4 Citations (Scopus)

Recent advances in the determination of G protein-coupled receptor structures

Thal, D. M., Vuckovic, Z., Draper-Joyce, C. J., Liang, Y-L., Glukhova, A., Christopoulos, A. & Sexton, P. M., 1 Aug 2018, In : Current Opinion in Structural Biology. 51, p. 28-34 7 p.

Research output: Contribution to journalArticleResearchpeer-review

20 Citations (Scopus)

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 & Translational Science. 1, 2, p. 73-83 11 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

Strength in numbers - An arrestin interaction code

Draper-Joyce, C. J. & Christopoulos, A., 1 Jun 2018, In : Nature Structural & Molecular Biology. 25, 6, p. 437-439 3 p.

Research output: Contribution to journalReview ArticleOtherpeer-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
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11 Citations (Scopus)

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

76 Citations (Scopus)

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

2 Citations (Scopus)

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 of the United States of America. 115, 10, p. E2419-E2428 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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21 Citations (Scopus)

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

93 Citations (Scopus)
3 Citations (Scopus)

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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6 Citations (Scopus)

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

8 Citations (Scopus)

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
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7 Citations (Scopus)