1993 …2023
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Research Output 1993 2020

4 Citations (Scopus)

Muscarinic acetylcholine receptors in the central nervous system: structure, function and pharmacology

Christopoulos, A., 2007, Exploring the Vertebrate Central Cholinergic Nervous System. Karczmar, A. G. (ed.). First ed. New York USA: Springer, p. 163 - 208 46 p.

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Researchpeer-review

9 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
85 Citations (Scopus)

New insights into the function of M4 muscarinic acetylcholine receptors gained using a novel allosteric modulator and a DREADD (designer receptor exclusively activated by a designer drug)

Nawaratne, O. V., Leach, K., Suratman, S., Loiacono, R., Felder, C. C., Armbruster, B. N., Roth, B. L., Sexton, P. & Christopoulos, A., 2008, In : Molecular Pharmacology. 74, 4, p. 1119 - 1131 13 p.

Research output: Contribution to journalArticleResearchpeer-review

13 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

Non-classical modes of signaling by 5HT(2C) receptors

Christopoulos, A., 2006, p. 55 - 55. 1 p.

Research output: Contribution to conferenceAbstractOther

7 Citations (Scopus)

Non-surmountable antagonism: Transcending steady state [3]

Lew, M. J., Christopoulos, A. & Ziogas, J., 1 Feb 2001, In : Trends in Pharmacological Sciences. 22, 2, p. 65-66 2 p.

Research output: Contribution to journalLetterOtherpeer-review

85 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

8 Citations (Scopus)

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

34 Citations (Scopus)

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

7 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

18 Citations (Scopus)

Novel persistent activation of muscarinic M1 receptors by xanomeline

Christopoulos, A. & El-Fakahany, E. E., 3 Sep 1997, In : European Journal of Pharmacology. 334, 1, p. R3-R4 2 p.

Research output: Contribution to journalArticleOtherpeer-review

219 Citations (Scopus)

Novel receptor partners and function of receptor activity-modifying proteins

Christopoulos, A., Christopoulos, G., Morfis, M., Udawela, M., Laburthe, M., Couvineau, A., Kuwasako, K., Tilakaratne, N. & Sexton, P. M., 2003, In : Journal of Biological Chemistry. 278, 5, p. 3293 - 3297 5 p.

Research output: Contribution to journalArticleResearchpeer-review

38 Citations (Scopus)

On the mechanism of interaction of potent surmountable and insurmountable antagonists with the prostaglandin D2 receptor CRTH2

Mathiesen, J. M., Christopoulos, A., Ulven, T., Royer, J. F., Campillo, M., Heinemann, A., Pardo, L. & Kostenis, E., 2006, In : Molecular Pharmacology. 69, 4, p. 1441 - 1453 13 p.

Research output: Contribution to journalArticleResearchpeer-review

50 Citations (Scopus)

On the unique binding and activating properties of xanomeline at the M1 muscarinic acetylcholine receptor

Christopoulos, A., Pierce, T. L., Sorman, J. L. & El-Fakahany, E. E., 1 Jun 1998, In : Molecular Pharmacology. 53, 6, p. 1120-1130 11 p.

Research output: Contribution to journalArticleResearchpeer-review

69 Citations (Scopus)

Orthosteric/allosteric bitopic ligands going hybrid with GPCRs

Valant, C., Sexton, P. M. & Christopoulos, A., 1 Jun 2009, In : Molecular Interventions. 9, 3, p. 125-135 11 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

51 Citations (Scopus)

Orthosteric and allosteric modes of interaction of novel selective agonists of the M1 muscarinic acetylcholine receptor

Avlani, V. A., Langmead, C. J., Guida, E., Wood, M. D., Tehan, B. G., Herdon, H. J., Watson, J. M., Sexton, P. & Christopoulos, A., 2010, In : Molecular Pharmacology. 78, 1, p. 94 - 104 11 p.

Research output: Contribution to journalArticleResearchpeer-review

27 Citations (Scopus)

Overview of receptor allosterism

Gregory, K., Sexton, P. & Christopoulos, A., Dec 2010, In : Current Protocols in Pharmacology. Chapter 1, Supp 51, p. 1.21-1 - 1.21-34 1 p.

Research output: Contribution to journalArticleResearchpeer-review

43 Citations (Scopus)

Pharmacological analysis of cannabinoid receptor activity in the rat vas deferens

Christopoulos, A., Coles, P., Lay, L., Lew, M. J. & Angus, J. A., 1 Jan 2001, In : British Journal of Pharmacology. 132, 6, p. 1281-1291 11 p.

Research output: Contribution to journalArticleResearchpeer-review

17 Citations (Scopus)

Pharmacological analysis of the mode of interaction of McN-A-343 at atrial muscarinic M2 receptors

Christopoulos, A. & Mitchelson, F., 1997, In : European Journal of Pharmacology. p. 153 - 156 4 p.

Research output: Contribution to journalArticleResearchpeer-review

22 Citations (Scopus)

Pharmacological analysis of the novel mode of interaction between xanomeline and the M1 muscarinic acetylcholine receptor

Christopoulos, A., Parsons, A. M. & El-Fakahany, E. E., 1 Jun 1999, In : Journal of Pharmacology and Experimental Therapeutics. 289, 3, p. 1220-1228 9 p.

Research output: Contribution to journalArticleResearchpeer-review

129 Citations (Scopus)

Pharmacological discrimination of calcitonin receptor: receptor activity-modifying protein complexes

Hay, D. L., Christopoulos, G., Christopoulos, A., Poyner, D. R. & Sexton, P. M., 2005, In : Molecular Pharmacology. 67, 5, p. 1655 - 1665 11 p.

Research output: Contribution to journalArticleResearchpeer-review

14 Citations (Scopus)

Pharmacology of 5HT2C receptor-mediated ERK1/2 phosphorylation: Agonist-specific activation pathways and the impact of RNA editing

Werry, T. D., Stewart, G. D., Crouch, M. F., Watts, A., Sexton, P. & Christopoulos, A., 2008, In : Biochemical Pharmacology. 76, 10, p. 1276 - 1287 12 p.

Research output: Contribution to journalArticleResearchpeer-review

71 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
170 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

90 Citations (Scopus)

Polar transmembrane interactions drive formation of ligand-specific and signal pathway-biased family B G protein-coupled receptor conformations

Wootten, D. L., Simms, J. W., Miller, L. J., Christopoulos, A. & Sexton, P., 2013, In : Proceedings of the National Academy of Sciences. 110, 13, p. 5211 - 5216 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
1 Citation (Scopus)
49 Citations (Scopus)

Polymorphism and ligand dependent changes in human glucagon-like peptide-1 receptor (GLP-1R) function: allosteric rescue of loss of function mutation

Koole, C., Wootten, D., Simms, J., Valant, C., Miller, L. J., Christopoulos, A. & Sexton, P., 2011, In : Molecular Pharmacology. 80, 3, p. 486 - 497 12 p.

Research output: Contribution to journalArticleResearchpeer-review

7 Citations (Scopus)
106 Citations (Scopus)

Positive and negative allosteric modulators promote biased signaling at the calcium-sensing receptor

Davey, A. E., Leach, K., Valant, C., Conigrave, A. D., Sexton, P. M. & Christopoulos, A., 2012, In : Endocrinology. 153, 3, p. 1232 - 1241 10 p.

Research output: Contribution to journalArticleResearchpeer-review

17 Citations (Scopus)
5 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

Preface

Fryer, A. D., Christopoulos, A. & Nathanson, N. M., 2012, Muscarinic Receptors. Vol. 208. (Handbook of Experimental Pharmacology; vol. 208).

Research output: Chapter in Book/Report/Conference proceedingForeword / PostscriptOtherpeer-review

Preface

Christopoulos, A., 1 Jan 2000, Biomedical Applications of Computer Modeling. 1st ed. Boca Raton: CRC Press, p. vii 1 p.

Research output: Chapter in Book/Report/Conference proceedingForeword / PostscriptOtherpeer-review

Preface

Sexton, P. M. & Christopoulos, A., 12 Jul 2004, In : Current Pharmaceutical Design. 10, 17, p. xxx 1 p.

Research output: Contribution to journalEditorialOtherpeer-review

78 Citations (Scopus)
13 Citations (Scopus)

Probing structural requirements of positive allosteric modulators of the M4 muscarinic receptor

Huynh, T., Valant, C., Crosby, I. T., Sexton, P., Christopoulos, A. & Capuano, B., 2013, In : Journal of Medicinal Chemistry. 56, 20, p. 8196 - 8200 5 p.

Research output: Contribution to journalArticleResearchpeer-review

2 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
88 Citations (Scopus)

Probing the molecular mechanism of interaction between 4-n-butyl-1-[4-(2- methylphenyl)-4-oxo-1-butyl]-piperidine (AC-42) and the muscarinic M1 receptor: Direct pharmacological evidence that AC-42 is an allosteric agonist

Langmead, C. J., Fry, V. A., Forbes, I. T., Branch, C. L., Christopoulos, A., Wood, M. D. & Herdon, H. J., 2006, In : Molecular Pharmacology. 69, 1, p. 236 - 246 11 p.

Research output: Contribution to journalArticleResearchpeer-review

34 Citations (Scopus)

Procalcitonin has bioactivity at calcitonin receptor family complexes: Potential mediator implications in sepsis

Sexton, P., Christopoulos, G., Christopoulos, A., Nylen, E. S., Snider Jr., R. H. & Becker, K. L., 2008, In : Critical Care Medicine. 36, 5, p. 1637 - 1640 4 p.

Research output: Contribution to journalArticleResearchpeer-review

29 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
File
7 Citations (Scopus)

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

26 Citations (Scopus)

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

43 Citations (Scopus)

Qualitative and quantitative assessment of relative agonist efficacy

Christopoulos, A. & El-Fakahany, E. E., 1 Sep 1999, In : Biochemical Pharmacology. 58, 5, p. 735-748 14 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

28 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

10 Citations (Scopus)

Quantification of allosteric interactions at G protein-coupled receptors using radioligand binding assays

Leach, K., Sexton, P. & Christopoulos, A., 2011, In : Current Protocols in Pharmacology. 1, Supp 52 (Unit 1.22), p. 1 - 41 41 p.

Research output: Contribution to journalArticleResearchpeer-review

49 Citations (Scopus)

Quantification of functional selectivity at the human {alpha}1A-adrenoceptor

Evans, B. A., Broxton, N., Merlin, J., Sato, M., Hutchinson, D. S., Christopoulos, A. & Summers, R. J., 2011, In : Molecular Pharmacology. 79, 2, p. 298 - 307 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Quantification of functional selectivity at the human α1A- adrenoceptor (Molecular Pharmacology (2011) 79, (298-307))

Evans, B. A., Broxton, N., Merlin, J., Sato, M., Hutchinson, D. S., Christopoulos, A. & Summers, R. J., Mar 2011, In : Molecular Pharmacology. 79, 3, p. 627 1 p.

Research output: Contribution to journalComment / DebateOtherpeer-review

107 Citations (Scopus)

Quantification of ligand bias for clinically relevant beta2-adrenergic receptor ligands: Implications for drug taxonomy

van der Westhuizen, E. T., Breton, B., Christopoulos, A. & Bouvier, M., 2014, In : Molecular Pharmacology. 85, 3, p. 492 - 509 18 p.

Research output: Contribution to journalArticleResearchpeer-review

82 Citations (Scopus)

RAMPs: 5 years on, where to now?

Morfis, M., Christopoulos, A. & Sexton, P., 2003, In : Trends in Pharmacological Sciences. 24, 11, p. 596 - 601 6 p.

Research output: Contribution to journalArticleResearchpeer-review

9 Citations (Scopus)

RAMPs as drug targets

Sexton, P. M., Poyner, D. R., Simms, J., Christopoulos, A. & Hay, D. L., 2012, RAMPs. Spielman, W. S. & Parameswaran, N. (eds.). 1st ed. USA: Springer, p. 61 - 74 14 p.

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Researchpeer-review