1993 …2023
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Research Output 1993 2019

2013

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

Recent advances in understanding GLP-1R (glucagon-like peptide-1 receptor) function

Koole, C. R., Pabreja, K., Savage, E. E., Wootten, D. L., Furness, S. G. B., Miller, L. J., Christopoulos, A. & Sexton, P., 2013, In : Biochemical Society Transactions. 41, 1, p. 172 - 179 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Signalling bias in new drug discovery: detection, quantification and therapeutic impact

Kenakin, T. & Christopoulos, A., 2013, In : Nature Reviews Drug Discovery. 12, 3, p. 205 - 216 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Structural basis for modulation of a G-protein-coupled receptor by allosteric drugs

Dror, R., Green, H. F., Valant, C., Borhani, D. W., Valcourt, J. R., Pan, A. C., Arlow, D. H., Canals, M., Lane, J. R. D., Rahmani, R. S., Baell, J. B., Sexton, P., Christopoulos, A. & Shaw, D. E., 2013, In : Nature. 503, 7475, p. 295 - 299 5 p.

Research output: Contribution to journalArticleResearchpeer-review

Supra-physiological efficacy at GPCRs: superstition or super agonists?

Langmead, C. J. & Christopoulos, A., 2013, In : British Journal of Pharmacology. 169, 2, p. 353 - 356 4 p.

Research output: Contribution to journalArticleOtherpeer-review

Tyrosine sulfation of chemokine receptor CCR2 enhances interactions with both monomeric and dimeric forms of the chemokine monocyte chemoattractant protein-1 (MCP-1)

Tan Hoong Yu, J., Ludeman, J. P., Wedderburn, J., Canals, M., Hall, P. H., Butler, S. J., Taleski, D., Christopoulos, A., Hickey, M. J., Payne, R. J. & Stone, M. J., 2013, In : Journal of Biological Chemistry. 288, 14, p. 10024 - 10034 11 p.

Research output: Contribution to journalArticleResearchpeer-review

2012

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

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

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

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

Consequences of splice variation on secretin family G protein-coupled receptor function

Furness, S. G. B., Wootten, D. L., Christopoulos, A. & Sexton, P. M., 2012, In : British Journal of Pharmacology. 166, 1, p. 98 - 109 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File

Design and receptor interactions of obligate dimeric mutant of chemokine monocyte chemoattractant protein-1 (MCP-1)

Tan Hoong Yu, J., Canals, M., Ludeman, J. P., Wedderburn, J., Boston, C., Butler, S. J., Carrick, A. M., Parody, T. R., Taleski, D., Christopoulos, A., Payne, R. J. & Stone, M. J., 2012, In : Journal of Biological Chemistry. 287, 18, p. 14692 - 14702 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Glucagon-like peptide-1 receptor dimerization differentially regulates agonist signaling but does not affect small molecule allostery

Harikumar, K. G., Wootten, D. L., Pinon, D. I., Koole, C. R., Ball, A. M., Furness, S. GB., Graham, B., Dong, M., Christopoulos, A., Miller, L. J. & Sexton, P. M., 2012, In : Proceedings of the National Academy of Sciences. 109, 45, p. 18607 - 18612 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File

Identification of molecular phenotypes and biased signaling induced by naturally occurring mutations of the human calcium-sensing receptor

Leach, K., Wen, C., Davey, A. E., Sexton, P. M., Conigrave, A. D. & Christopoulos, A., 2012, In : Endocrinology. 153, 9, p. 4304 - 4316 13 p.

Research output: Contribution to journalArticleResearchpeer-review

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

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

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

Second extracellular loop of human glucagon-like peptide-1 receptor (GLP-1R) differentially regulates orthosteric but not allosteric agonist binding and function

Koole, C. R., Wootten, D. L., Simms, J., Savage, E. E., Miller, L. J., Christopoulos, A. & Sexton, P. M., 2012, In : Journal of Biological Chemistry. 287, 6, p. 3659 - 3673 15 p.

Research output: Contribution to journalArticleResearchpeer-review

Second extracellular loop of human glucagon-like peptide-1 receptor (GLP-1R) has a critical role in GLP-1 peptide binding and receptor activation

Koole, C. R., Wootten, D. L., Simms, J. W., Miller, L. J., Christopoulos, A. & Sexton, P., 2012, In : Journal of Biological Chemistry. 287, 6, p. 3642 - 3658 17 p.

Research output: Contribution to journalArticleResearchpeer-review

Small molecule allosteric modulation of the glucagon-like Peptide-1 receptor enhances the insulinotropic effect of oxyntomodulin

Willard, F. S., Wootten, D. L., Showalter, A. D., Savage, E. E., Ficorilli, J., Farb, T. B., Bokvist, K., Alsina-Fernandez, J., Furness, S. GB., Christopoulos, A., Sexton, P. M. & Sloop, K. W., 2012, In : Molecular Pharmacology. 82, 6, p. 1066 - 1073 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Stimulus bias provides evidence for conformational constraints in the structure of a G protein-coupled receptor

Gregory, K. J., Sexton, P. M., Tobin, A. B. & Christopoulos, A., 2012, In : Journal of Biological Chemistry. 287, 44, p. 37066 - 37077 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Structure-function studies of muscarinic acetylcholine receptors

Leach, K., Simms, J., Sexton, P. M. & Christopoulos, A., 2012, Muscarinic Receptors - Handbook of Experimental Pharmacology 208. Fryer, A. D., Christopoulos, A. & Nathanson, N. M. (eds.). 1st ed. USA: Springer, p. 29 - 48 20 p.

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Other

Synthesis and characterization of novel 2-amino-3-benzoylthiophene derivatives as biased allosteric agonists and modulators of the adenosine A1 receptor

Valant, C., Aurelio, L., Devine, S. M., Ashton, T. D., White, J. M., Sexton, P. M., Christopoulos, A. & Scammells, P. J., 2012, In : Journal of Medicinal Chemistry. 55, 5, p. 2367 - 2375 9 p.

Research output: Contribution to journalArticleResearchpeer-review

Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6- tetrahydropyridines as 5-HT2C agonists

Conway, R., Valant, C., Christopoulos, A., Robertson, A. D., Capuano, B. & Crosby, I. T., 2012, In : Bioorganic and Medicinal Chemistry Letters. 22, 7, p. 2560 - 2564 5 p.

Research output: Contribution to journalArticleResearchpeer-review

The best of both worlds? Bitopic orthosteric/allosteric ligands of G protein - coupled receptors

Valant, C., Lane, J., Sexton, P. & Christopoulos, A., 2012, In : Annual Review of Pharmacology and Toxicology. 53, p. 153 - 178 26 p.

Research output: Contribution to journalArticleResearchpeer-review

2011

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

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

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

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

Impact of species variability and "probe-dependence" on the detection and in vivo validation of allosteric modulation at the M(4) muscarinic acetylcholine receptor

Suratman, N. S., Leach, K., Sexton, P., Felder, C. C., Loiacono, R. & Christopoulos, A., 2011, In : British Journal of Pharmacology. 162, 7, p. 1659 - 1670 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Ligand functional selectivity and quantitative pharmacology at G protein-coupled receptors

Stallaert, W., Christopoulos, A. & Bouvier, M., 2011, In : Expert Opinion on Drug Discovery. 6, 8, p. 811 - 825 15 p.

Research output: Contribution to journalArticleResearchpeer-review

Modulation of the glucagon-like peptide-1 receptor signaling by naturally occurring and synthetic flavonoids

Wootten, D., Simms, J., Koole, C., Woodman, O., Summers, R., Christopoulos, A. & Sexton, P., 2011, In : Journal of Pharmacology and Experimental Therapeutics. 336, 2, p. 540 - 550 11 p.

Research output: Contribution to journalArticleResearchpeer-review

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

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

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

Relative affinity of angiotensin peptides and novel ligands at AT1 and AT2 receptors

Bosnyak, S., Jones, E., Christopoulos, A., Aguilar, M., Thomas, W. & Widdop, R., 2011, In : Clinical Science. 121, 7, p. 297 - 303 7 p.

Research output: Contribution to journalArticleResearchpeer-review

The role of transmembrane domain 3 (Tmiii) in the actions of orthosteric, allosteric and atypical agonists of the M4 muscarinic acetylcholine receptor

Leach, K., Davey, A. E., Felder, C. C., Sexton, P. & Christopoulos, A., 2011, In : Molecular Pharmacology. 79, 5, p. 855 - 865 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Delineating the mode of action of adenosine A1 receptor allosteric modulators

Valant, C., Aurelio, L., Urmaliya, V., White, P., Scammells, P., Sexton, P. & Christopoulos, A., 2010, In : Molecular Pharmacology. 78, 3, p. 444 - 455 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Detection of novel functional selectivity at M3 muscarinic acetylcholine receptors using a Saccharomyces cerevisiae platform

Stewart, G. D., Sexton, P. & Christopoulos, A., 2010, In : ACS Chemical Biology. 5, 4, p. 365 - 375 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Effects of conformational restriction of 2-amino-3-benzoylthiophenes on A1 adenosine receptor modulation

Aurelio, L., Valant, C., Flynn, B., Sexton, P., White, J., Christopoulos, A. & Scammells, P., 2010, In : Journal of Medicinal Chemistry. 53, p. 6550 - 6559 10 p.

Research output: Contribution to journalArticleResearchpeer-review

H2 relaxin is a biased ligand relative to H3 relaxin at the relaxin family peptide receptor 3 (RXFP3) [S]

van der Westhuizen, E. T., Christopoulos, A., Sexton, P., Wade, J. & Summers, R., 2010, In : Molecular Pharmacology. 77, 5, p. 759 - 772 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Identification of orthosteric and allosteric site mutations in M 2 muscarinic acetylcholine receptors that contribute to ligand-selective signaling bias

Gregory, K. J., Hall, N., Tobin, A., Sexton, P. & Christopoulos, A., 2010, In : Journal of Biological Chemistry. 285, 10, p. 7459 - 7474 16 p.

Research output: Contribution to journalArticleResearchpeer-review

Measurement of ligand-G protein-coupled receptor interactions

Leach, K., Valant, C., Sexton, P. M. & Christopoulos, A., 25 Jan 2010, G Protein-Coupled Receptors: Essential Methods. Poyner, D. R. & Wheatley, M. (eds.). Chichester UK: Wiley-Blackwell, p. 1-29 29 p. (Proteins & Macromolecules).

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