1993 …2023
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Research Output 1993 2020

2011
21 Citations (Scopus)

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

2012
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

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

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

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

27 Citations (Scopus)

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
31 Citations (Scopus)

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

38 Citations (Scopus)

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
46 Citations (Scopus)

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

1 Citation (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

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

78 Citations (Scopus)
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

19 Citations (Scopus)

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

56 Citations (Scopus)

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

30 Citations (Scopus)

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

22 Citations (Scopus)

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

13 Citations (Scopus)

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

34 Citations (Scopus)

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

5 Citations (Scopus)

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

113 Citations (Scopus)

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

2013
471 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

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

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
61 Citations (Scopus)

A structure-activity analysis of biased agonism at the dopamine D2 receptor

Shonberg, J., Klein Herenbrink, C., Lopez, L., Christopoulos, A., Scammells, P. J., Capuano, B. & Lane, J. R. D., 2013, In : Journal of Medicinal Chemistry. 56, 22, p. 9199 - 9221 23 p.

Research output: Contribution to journalArticleResearchpeer-review

92 Citations (Scopus)

Bridging the gap: bitopic ligands of G-protein-coupled receptors

Lane, J. R. D., Sexton, P. M. & Christopoulos, A., 2013, In : Trends in Pharmacological Sciences. 34, 1, p. 59 - 66 8 p.

Research output: Contribution to journalArticleResearchpeer-review

22 Citations (Scopus)

Calcium-sensing receptor-dependent activation of CREB phosphorylation in HEK293 cells and human parathyroid cells

Avlani, V. A., Ma, W., Mun, H., Leach, K., Delbridge, L., Christopoulos, A. & Conigrave, A., 2013, In : American Journal of Physiology - Endocrinology and Metabolism. 304, 10, p. 1097 - 1104 8 p.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

CGRP/adrenomedullin

Wootten, D. L., Tilakaratne, N., Christopoulos, A. & Sexton, P., 2013, Handbook of Biologically Active Peptides. Kastin, A. J. (ed.). Second Edition ed. San Diego CA USA: Elsevier, p. 744 - 751 8 p.

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

53 Citations (Scopus)

Development of M1 mAChR allosteric and bitopic ligands: Prospective therapeutics for the treatment of cognitive deficits

Davie, B. J., Christopoulos, A. & Scammells, P. J., 2013, In : ACS Chemical Neuroscience. 4, 7, p. 1026 - 1048 23 p.

Research output: Contribution to journalArticleResearchpeer-review

50 Citations (Scopus)

Differential activation and modulation of the glucagon-like peptide-1 receptor by small molecule ligands

Wootten, D. L., Savage, E. E., Willard, F. S., Bueno, A. B., Sloop, K. W., Christopoulos, A. & Sexton, P., 2013, In : Molecular Pharmacology. 83, 4, p. 822 - 834 13 p.

Research output: Contribution to journalArticleResearchpeer-review

223 Citations (Scopus)

Emerging paradigms in GPCR allostery: implications for drug discovery

Wootten, D. L., Christopoulos, A. & Sexton, P., 2013, In : Nature Reviews Drug Discovery. 12, 8, p. 630 - 644 15 p.

Research output: Contribution to journalArticleResearchpeer-review

Erratum: Differential activation and modulation of the glucagon-like peptide-1 receptor by small molecular ligands (Molecular Pharmacology (2013) 83 (822-834))

Wootten, D., Savage, E. E., Willard, F. S., Bueno, A. B., Sloop, K. W., Christopoulos, A. & Sexton, P. M., Jul 2013, In : Molecular Pharmacology. 84, 1, p. 170 1 p.

Research output: Contribution to journalComment / DebateOtherpeer-review

17 Citations (Scopus)

Impact of chronic congestive heart failure on pharmacokinetics and vasomotor effects of infused nitrite

Maher, A. R., Arif, S., Madhani, M., Abozguia, K., Ahmed, I., Fernandez, B. O., Feelisch, M., O'Sullivan, A. G., Christopoulos, A., Sverdlov, A. L., Ngo, D., Dautov, R., James, P. E., Horowitz, J. D. & Frenneaux, M. P., 2013, In : British Journal of Pharmacology. 169, 3, p. 659 - 670 12 p.

Research output: Contribution to journalArticleResearchpeer-review

48 Citations (Scopus)

Impact of clinically relevant mutations on the pharmacoregulation and signaling bias of the calcium-sensing receptor by positive and negative allosteric modulators

Leach, K., Wen, C., Cook, A. E., Sexton, P., Conigrave, A. & Christopoulos, A., 2013, In : Endocrinology. 154, 3, p. 1105 - 1116 12 p.

Research output: Contribution to journalArticleResearchpeer-review

86 Citations (Scopus)

Inhibition of tumor angiogenesis and growth by a small-molecule multi-FGF receptor blocker with allosteric properties

Bono, F., De Smet, F., Herbert, C., De Bock, K., Georgiadou, M., Fons, P., Tjwa, M., Alcouffe, C., Ny, A., Bianciotto, M., Jonckx, B., Murakami, M., Lanahan, A. A., Michielsen, C., Sibrac, D., Dol-Gleizes, F., Mazzone, M., Zacchigna, S., Herault, J-P., Fischer, C. & 33 others, Rigon, P., Ruiz de Almodovar, C., Claes, F., Blanc, I., Poesen, K., Zhang, Z., Segura, I., Gueguen, G., Bordes, M-F., Lambrechts, D., Broussy, R., van de Wouwer, M., Michaux, C., Shimada, T., Jean, I., Blacher, S., Noel, A., Motte, P., Rom, E., Rakic, J-M., Katsuma, S., Schaeffer, P., Yayon, A., Van Schepdael, A., Schwalbe, H., Gervasio, F. L., Carmeliet, G., Rozensky, J., Dewerchin, M., Simons, M., Christopoulos, A., Herbert, J-M. & Carmeliet, P., 2013, In : Cancer Cell. 23, 4, p. 477 - 488 12 p.

Research output: Contribution to journalArticleResearchpeer-review

37 Citations (Scopus)

Measurements of ligand bias and functional affinity

Kenakin, T. & Christopoulos, A., 2013, In : Nature Reviews Drug Discovery. 12, 6, p. 483 - 483 1 p.

Research output: Contribution to journalLetterOther

23 Citations (Scopus)

Minireview: Signal bias, allosterism, and polymorphic variation at the GLP-1R: implications for drug discovery

Koole, C. R., Savage, E. E., Christopoulos, A., Miller, L. J., Sexton, P. & Wootten, D. L., 2013, In : Molecular Endocrinology. 27, 8, p. 1234 - 1244 11 p.

Research output: Contribution to journalArticleResearchpeer-review

11 Citations (Scopus)

Molecular basis for benzodiazepine agonist action at the type 1 cholecystokinin receptor

Harikumar, K. G., Cawston, E. E., Lam, P. C. H., Patil, A., Orry, A., Henke, B., Abagyan, R., Christopoulos, A., Sexton, P. & Miller, L. J., 2013, In : Journal of Biological Chemistry. 288, 29, p. 21082 - 21095 14 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
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

44 Citations (Scopus)

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

421 Citations (Scopus)

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

245 Citations (Scopus)

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

20 Citations (Scopus)

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

48 Citations (Scopus)

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

2014
109 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