1993 …2023
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Research Output 1993 2019

4 Citations (Scopus)

[3H]N-methylscopolamine dissociation from muscarine receptors affected by low concentrations of allosteric modulators

Christopoulos, A. & Mitchelson, F., 15 Aug 1995, In : European Journal of Pharmacology: Molecular Pharmacology. 290, 3, p. 259-262 4 p.

Research output: Contribution to journalArticleResearchpeer-review

38 Citations (Scopus)

2-Aminothienopyridazines as novel adenosine A1 receptor allosteric modulators and antagonists

Ferguson, G. N., Valant, C., Horne, H. J., Figler, H., Flynn, B. L., Linden, J., Chalmers, D. K., Sexton, P., Christopoulos, A. & Scammells, P. J., 2008, In : Journal of Medicinal Chemistry. 51, 19, p. 6165 - 6172 8 p.

Research output: Contribution to journalArticleResearchpeer-review

26 Citations (Scopus)

3- and 6-substituted 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridines as A1 adenosine receptor allosteric modulators and antagonists

Aurelio, L., Valant, C., Figler, H., Flynn, B. L., Linden, J., Sexton, P., Christopoulos, A. & Scammells, P. J., 2009, In : Bioorganic & Medicinal Chemistry. 17, 20, p. 7353 - 7361 9 p.

Research output: Contribution to journalArticleResearchpeer-review

20 Citations (Scopus)

4-phenylpyridin-2-one derivatives: a novel class of positive allosteric modulator of the M1 muscarinic acetylcholine receptor

Mistry, S. N., Jorg, M., Lim, H., Vinh, N. B., Sexton, P. M., Capuano, B., Christopoulos, A., Lane, J. R. & Scammells, P. J., 14 Jan 2016, In : Journal of Medicinal Chemistry. 59, 1, p. 388-409 22 p.

Research output: Contribution to journalArticleResearchpeer-review

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

34 Citations (Scopus)

Accelerated structure-based design of chemically diverse allosteric modulators of a muscarinic G protein-coupled receptor

Miao, Y., Goldfeld, D. A., Moo, E. V., Sexton, P. M., Christopoulos, A., McCammon, J. A. & Valant, C., 20 Sep 2016, In : Proceedings of the National Academy of Sciences. 113, 38, p. E5675-E5684 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access

A common site of action for two allosteric antagonists

Christopoulos, A., Lanzafame, A. & Mitchelson, F. J., 1997, p. 1173 - 1173. 1 p.

Research output: Contribution to conferenceAbstractOther

29 Citations (Scopus)

A critical role for the short intracellular C terminus in receptor activity-modifying protein function

Udawela, M., Christopoulos, G., Morfis, M., Christopoulos, A., Ye, S., Tilakaratne, N. & Sexton, P. M., 2006, In : Molecular Pharmacology. 70, 5, p. 1750 - 1760 11 p.

Research output: Contribution to journalArticleResearchpeer-review

466 Citations (Scopus)

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

107 Citations (Scopus)

Advances in G protein-coupled receptor allostery: From function to structure

Christopoulos, A., 2014, In : Molecular Pharmacology. 86, 5, p. 463 - 478 16 p.

Research output: Contribution to journalArticleResearchpeer-review

25 Citations (Scopus)

A hydrogen-bonded polar network in the core of the glucagon-like peptide-1 receptor is a fulcrum for biased agonism: lessons from class B crystal structuress

Wootten, D., Reynolds, C. A., Koole, C., Smith, K. J., Mobarec, J. C., Simms, J., Quon, T., Coudrat, T., Furness, S. G. B., Miller, L. J., Christopoulos, A. & Sexton, P. M., 1 Mar 2016, In : Molecular Pharmacology. 89, 3, p. 335-347 13 p.

Research output: Contribution to journalArticleResearchpeer-review

40 Citations (Scopus)

A kinetic view of GPCR allostery and biased agonism

Lane, J. R., May, L. T., Parton, R. G., Sexton, P. M. & Christopoulos, A., 18 Aug 2017, In : Nature Chemical Biology. 13, 9, p. 929-937 9 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

Open Access
File
103 Citations (Scopus)

Allosteric agonists of 7TM receptors: expanding the pharmacological toolbox

Langmead, C. J. & Christopoulos, A., 2006, In : Trends in Pharmacological Sciences. 27, 9, p. 475 - 481 7 p.

Research output: Contribution to journalArticleResearchpeer-review

487 Citations (Scopus)

Allosteric binding sites on cell-surface receptors: Novel targets for drug discovery

Christopoulos, A., 1 Mar 2002, In : Nature Reviews Drug Discovery. 1, 3, p. 198-210 13 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

246 Citations (Scopus)

Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology

Leach, K., Sexton, P. & Christopoulos, A., 2007, In : Trends in Pharmacological Sciences. 28, 8, p. 382 - 389 8 p.

Research output: Contribution to journalArticleResearchpeer-review

92 Citations (Scopus)

Allosteric interactions at muscarinic cholinoceptors

Christopoulos, A., Lanzafame, A. & Mitchelson, F. J., 1998, In : Clinical and Experimental Pharmacology and Physiology. p. 185 - 194 10 p.

Research output: Contribution to journalArticleResearchpeer-review

128 Citations (Scopus)

Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner: Implications for drug screening

Koole, C., Wootten, D., Simms, J., Valant, C., Sridhar, R., Woodman, O., Miller, L. J., Summers, R., Christopoulos, A. & Sexton, P. M., 2010, In : Molecular Pharmacology. 78, 3, p. 456 - 465 10 p.

Research output: Contribution to journalArticleResearchpeer-review

8 Citations (Scopus)

Allosteric modulation as a unifying mechanism for receptor function and regulation

Changeux, J-P. & Christopoulos, A., 1 Sep 2017, In : Diabetes, Obesity and Metabolism. 19, p. 4-21 18 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

Open Access
File
78 Citations (Scopus)

Allosteric Modulation as a Unifying Mechanism for Receptor Function and Regulation

Changeux, J. P. & Christopoulos, A., 25 Aug 2016, In : Cell. 166, 5, p. 1084-1102 19 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

16 Citations (Scopus)

Allosteric modulation of a chemogenetically modified G protein-coupled receptor

Abdul Ridha, A., Lane, J. R. D., Sexton, P., Canals, M. & Christopoulos, A., 2013, In : Molecular Pharmacology. 83, 2, p. 521 - 530 10 p.

Research output: Contribution to journalArticleResearchpeer-review

3 Citations (Scopus)

Allosteric modulation of chemokine receptors

Tschammer, N., Christopoulos, A. & Kenakin, T., 2015, Chemokines: Chemokines and Their Receptors in Drug Discovery. Tschammer, N. (ed.). Cham Switzerland: Springer, p. 87-117 31 p.

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

48 Citations (Scopus)

Allosteric modulation of endogenous metabolites as an avenue for drug discovery

Wootten, D. L., Savage, E. E., Valant, C., May, L. T., Sloop, K. W., Ficorilli, J., Showalter, A. D., Willard, F. S., Christopoulos, A. & Sexton, P. M., 2012, In : Molecular Pharmacology. 82, 2, p. 281 - 290 10 p.

Research output: Contribution to journalArticleResearchpeer-review

69 Citations (Scopus)

Allosteric modulation of G protein-coupled receptors

May, L. T., Avlani, V. A., Sexton, P. M. & Christopoulos, A., 2004, In : Current Pharmaceutical Design. 10, 17, p. 2003-2013 11 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

474 Citations (Scopus)

Allosteric modulation of G protein-coupled receptors

May, L. T., Leach, K., Sexton, P. M. & Christopoulos, A., 2007, In : Annual Review of Pharmacology and Toxicology. 47, p. 1 - 51 51 p.

Research output: Contribution to journalArticleResearchpeer-review

Allosteric modulation of G protein-coupled receptors

May, L. T., Avlani, V. A., Sexton, P. & Christopoulos, A., 2004, In : Current Pharmaceutical Design. 10, 17, p. 2003 - 2013 11 p.

Research output: Contribution to journalArticleResearchpeer-review

194 Citations (Scopus)

Allosteric modulation of G protein-coupled receptors: A pharmacological perspective

Keov, P., Sexton, P. & Christopoulos, A., 2011, In : Neuropharmacology. 60, 1, p. 24 - 35 12 p.

Research output: Contribution to journalArticleResearchpeer-review

16 Citations (Scopus)

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

73 Citations (Scopus)

Allosteric modulation of muscarinic acetylcholine receptors

Gregory, K. J., Sexton, P. & Christopoulos, A., 2007, In : Current Neuropharmacology. 5, 3, p. 157 - 167 11 p.

Research output: Contribution to journalArticleResearchpeer-review

162 Citations (Scopus)

Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery

Melancon, B. J., Hopkins, C. R., Wood, M. R., Emmitte, K. A., Niswender, C. M., Christopoulos, A., Conn, P. J. & Lindsley, C. W., 2012, In : Journal of Medicinal Chemistry. 55, 4, p. 1445 - 1464 20 p.

Research output: Contribution to journalArticleResearchpeer-review

45 Citations (Scopus)

Allosteric modulation of the calcium-sensing receptor by gamma-glutamyl peptides inhibition of PTH secretion, suppression of intraceullar cAMP levels and a common mechanism of action with L-amino acids

Broadhead, G., Mun, H., Avlani, V., Jourdon, O., Church, W., Christopoulos, A., Delbridge, L. & Conigrave, A., 2011, In : Journal of Biological Chemistry. 286, 11, p. 8786 - 8797 12 p.

Research output: Contribution to journalArticleResearchpeer-review

292 Citations (Scopus)

Allosteric modulation of the cannabinoid CB1 receptor

Price, M. R., Baillie, G. L., Thomas, A., Stevenson, L. A., Easson, M., Goodwin, R., McLean, A., McIntosh, L., Goodwin, G., Walker, G., Westwood, P., Marrs, J., Thomson, F., Cowley, P., Christopoulos, A., Pertwee, R. G. & Ross, R. A., 2005, In : Molecular Pharmacology. 68, 5, p. 1484 - 1495 12 p.

Research output: Contribution to journalArticleResearchpeer-review

161 Citations (Scopus)

Allosteric modulation of the muscarinic M4 receptor as an approach to treating schizophrenia

Chan, W. Y., McKinzie, D. L., Bose, S., Mitchell, S. N., Witkin, J. M., Thompson, R. C., Christopoulos, A., Lazareno, S., Birdsall, N. JM., Bymaster, F. P. & Felder, C. C., 2008, In : Proceedings of the National Academy of Sciences. 105, 31, p. 10978 - 10983 6 p.

Research output: Contribution to journalArticleResearchpeer-review

664 Citations (Scopus)

Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders

Conn, P. J., Christopoulos, A. & Lindsley, C. W., 2009, In : Nature Reviews Drug Discovery. 8, 1, p. 41 - 54 14 p.

Research output: Contribution to journalArticleResearchpeer-review

64 Citations (Scopus)

Allosteric modulators of G-protein-coupled receptors

May, L. T. & Christopoulos, A., Oct 2003, In : Current Opinion in Pharmacology. 3, 5, p. 551-556 6 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

86 Citations (Scopus)
36 Citations (Scopus)

Allosteric targeting of receptor tyrosine kinases

De Smet, F., Christopoulos, A. & Carmeliet, P., 2014, In : Nature Biotechnology. 32, 11, p. 1113 - 1120 8 p.

Research output: Contribution to journalArticleResearchpeer-review

31 Citations (Scopus)

Allostery and Biased Agonism at Class B G Protein-Coupled Receptors

Wootten, D., Miller, L. J., Koole, C., Christopoulos, A. & Sexton, P. M., 11 Jan 2017, In : Chemical Reviews. 117, 1, p. 111-138 28 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

46 Citations (Scopus)

Allostery in GPCRs: 'MWC' revisited

Canals, M., Sexton, P. & Christopoulos, A., 2011, In : Trends in Biochemical Sciences. 36, 12, p. 663 - 672 10 p.

Research output: Contribution to journalArticleResearchpeer-review

84 Citations (Scopus)

A Monod-Wyman-Changeux mechanism can explain G protein-coupled receptor (GPCR) allosteric modulation

Canals, M., Lane, J., Wen, A., Scammells, P., Sexton, P. & Christopoulos, A., 2012, In : Journal of Biological Chemistry. 287, 1, p. 650 - 659 10 p.

Research output: Contribution to journalArticleResearchpeer-review

63 Citations (Scopus)

Amylin receptors: Molecular composition and pharmacology

Hay, D. L., Christopoulos, G., Christopoulos, A. & Sexton, P., 2004, In : Biochemical Society Transactions. 32, Pt 5, p. 865 - 867 3 p.

Research output: Contribution to journalArticleOther

23 Citations (Scopus)

Analytical pharmacology: the impact of numbers on pharmacology

Kenakin, T. & Christopoulos, A., 2011, In : Trends in Pharmacological Sciences. 32, 4, p. 189 - 196 8 p.

Research output: Contribution to journalArticleResearchpeer-review

77 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

129 Citations (Scopus)
14 Citations (Scopus)

A positive allosteric modulator of the adenosine A1 receptor selectively inhibits primary afferent synaptic transmission in a neuropathic pain model

Imlach, W. L., Bhola, R. F., May, L. T., Christopoulos, A. & Christie, M. J., 2015, In : Molecular Pharmacology. 88, 3, p. 460-468 9 p.

Research output: Contribution to journalArticleResearchpeer-review

15 Citations (Scopus)

Application of an allosteric ternary complex model to the technique of pharmacological resultant analysis

Christopoulos, A. & Mitchelson, F., 1997, In : Journal of Pharmacy and Pharmacology. p. 781 - 786 6 p.

Research output: Contribution to journalArticleResearchpeer-review

233 Citations (Scopus)

A simple method for quantifying functional selectivity and agonist bias

Kenakin, T., Watson, C., Muniz-Medina, V., Christopoulos, A. & Novick, S., 2012, In : ACS Chemical Neuroscience. 3, 3, p. 193 - 203 11 p.

Research output: Contribution to journalArticleResearchpeer-review

9 Citations (Scopus)

A simple method to generate stable cell lines for the analysis of transient protein-protein interactions

Savage, E. E., Wootten, D. L., Christopoulos, A., Sexton, P. & Furness, S. G. B., 2013, In : BioTechniques. 54, 4, p. 217 - 221 5 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
145 Citations (Scopus)

Assessing the distribution of parameters in models of ligand-receptor interaction: To log or not to log

Christopoulos, A., 1 Sep 1998, In : Trends in Pharmacological Sciences. 19, 9, p. 351-357 7 p.

Research output: Contribution to journalArticleResearchpeer-review

38 Citations (Scopus)

Assessment of the allosteric interactions of the bisquaternary heptane- 1,7-bis(dimethyl-3'-phthalimidopropyl)ammonium bromide at M1 and M2 muscarine receptors

Christopoulos, A. & Mitchelson, F., 1 Jan 1994, In : Molecular Pharmacology. 46, 1, p. 105-114 10 p.

Research output: Contribution to journalArticleResearchpeer-review