1993 …2023
If you made any changes in Pure these will be visible here soon.

Research Output 1993 2020

Filter
Article
2020

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
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

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
File

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 and Translational Sciences. 2, 3, p. 183-197 15 p.

Research output: Contribution to journalArticleResearchpeer-review

4 Citations (Scopus)

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
3 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

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

Mu and Delta Opioid Receptors are Co-expressed and Functionally Interact in the Enteric Nervous System of the Mouse Colon

Di Cello, J., Carbone, S., Saito, A., Rajasekhar, P., Ceredig, R. A., Pham, V., Valant, C., Christopoulos, A., Veldhuis, N. A., Canals, M., Massotte, D. & Poole, D. P., 20 Nov 2019, (Accepted/In press) In : Cellular and Molecular Gastroenterology and Hepatology. 47 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access

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

8 Citations (Scopus)
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
File
2 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

28 Citations (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

4 Citations (Scopus)
2 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

4 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

Open Access
File

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 and Translational Sciences. 1, 2, p. 96-109 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
8 Citations (Scopus)

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
File
5 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

2 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

10 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
File
79 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
File
3 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
File
15 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

8 Citations (Scopus)

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
2 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

15 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. 115, 10, p. E2419-E2428 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
69 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

5 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
File
7 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

7 Citations (Scopus)

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

5 Citations (Scopus)

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

2017
18 Citations (Scopus)

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

16 Citations (Scopus)

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

2 Citations (Scopus)

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

5 Citations (Scopus)

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
File
10 Citations (Scopus)

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

20 Citations (Scopus)

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 others, Tobin, 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
File
176 Citations (Scopus)

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

26 Citations (Scopus)

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
File
3 Citations (Scopus)

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

File
6 Citations (Scopus)

Structure-Based Design and Discovery of New M2 Receptor Agonists

Fish, I., Stößel, A., Eitel, K., Valant, C., Albold, S., Huebner, H., Möller, D., Clark, M. J., Sunahara, R. K., Christopoulos, A., Shoichet, B. K. & Gmeiner, P., 22 Nov 2017, In : Journal of Medicinal Chemistry. 60, 22, p. 9239-9250 12 p.

Research output: Contribution to journalArticleResearchpeer-review

87 Citations (Scopus)

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

431 Citations (Scopus)

The concise guide to Pharmacology 2017/18: G protein-coupled receptors

CGTP Collaborators, 1 Dec 2017, In : British Journal of Pharmacology. 174, p. S17-S129

Research output: Contribution to journalArticleOtherpeer-review

Open Access