1993 …2023
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Research Output 1993 2019

2003

Guest editor's introduction

Christopoulos, A., 15 Sep 2003, In : Receptors and Channels. 9, 4, p. 213-214 2 p.

Research output: Contribution to journalEditorialOtherpeer-review

328 Citations (Scopus)

International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification. XXXVIII. Update on Terms and Symbols in Quantitative Pharmacology

Neubig, R. R., Spedding, M., Kenakin, T. & Christopoulos, A., 1 Dec 2003, In : Pharmacological Reviews. 55, 4, p. 597-606 10 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

218 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

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

2004

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

70 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

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

16 Citations (Scopus)

Effects of anandamide on the binding and signaling properties of M 1 muscarinic acetylcholine receptors

Lanzafame, A. A., Guida, E. & Christopoulos, A., 1 Dec 2004, In : Biochemical Pharmacology. 68, 11, p. 2207-2219 13 p.

Research output: Contribution to journalArticleResearchpeer-review

41 Citations (Scopus)

G-protein-coupled receptor allosterism: the promise and the problem(s)

Christopoulos, A., May, L. T., Avlani, V. A. & Sexton, P. M., 2004, In : Biochemical Society Transactions. 32, Pt 5, p. 873 - 877 5 p.

Research output: Contribution to journalArticleOther

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

15 Citations (Scopus)

Regulation of serotonin 5-HT{2C} receptors by chronic ligand exposure

Devlin, M. G., Smith, N. J., Ryan, O. M., Guida, E., Sexton, P. M. & Christopoulos, A., 2004, In : European Journal of Pharmacology. 498, 1-3, p. 59 - 69 11 p.

Research output: Contribution to journalArticleResearchpeer-review

2005
295 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

68 Citations (Scopus)

Characterization of serotonin 5-HT2C receptor signaling to extracellular signal-regulated kinases 1 and 2

Werry, T. D., Gregory, K. J., Sexton, P. M. & Christopoulos, A., 2005, In : Journal of Neurochemistry. 93, p. 1603 - 1615 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Editorial

Christopoulos, A., 1 Jun 2005, In : Mini-Reviews in Medicinal Chemistry. 5, 6, p. 521-521 1 p.

Research output: Contribution to journalEditorialOtherpeer-review

8 Citations (Scopus)

Effects of urea pretreatment on the binding properties of adenosine A 1 receptors

May, L. T., Sexton, P. M. & Christopoulos, A., 2005, In : British Journal of Pharmacology. 146, 8, p. 1119 - 1129 11 p.

Research output: Contribution to journalArticleResearchpeer-review

268 Citations (Scopus)

G-protein-coupled receptor Mas is a physiological antagonist of the angiotensin II type 1 receptor

Kostenis, E., Milligan, G., Christopoulos, A., Sanchez-Ferrer, C. F., Heringer-Walther, S., Sexton, P. M., Gembardt, F., Kellett, E., Martini, L., Vanderheyden, P., Schultheiss, H-P. & Walther, T., 2005, In : Circulation. 111, p. 1806 - 1813 8 p.

Research output: Contribution to journalArticleResearchpeer-review

76 Citations (Scopus)

'Ins and outs' of seven-transmembrane receptor signalling to ERK

Werry, T. D., Sexton, P. M. & Christopoulos, A., 2005, In : Trends in Endocrinology and Metabolism. 16, 1, p. 26 - 33 8 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

28 Citations (Scopus)
2006
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

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

69 Citations (Scopus)

Complexing receptor pharmacology: modulation of family B G protein-coupled receptor function by RAMPs

Sexton, P., Morfis, M., Tilakaratne, N., Hay, D. L., Udawela, M., Christopoulos, G. & Christopoulos, A., 2006, In : Annals of the New York Academy of Sciences. 1070, p. 90 - 104 15 p.

Research output: Contribution to journalArticleResearchpeer-review

42 Citations (Scopus)

Distinct receptor activity-modifying protein domains differentially modulate interaction with calcitonin receptors

Udawela, M., Christopoulos, G., Tilakaratne, N., Christopoulos, A., Albiston, A. L. & Sexton, P. M., 2006, In : Molecular Pharmacology. 69, 6, p. 1984 - 1989 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Effective GPCR screening using ERK 1/2: applying SureFire to detect ERK 1/2 phosphorylation

Osmond, R. W., Dyer, A. R., Sexton, P. M., Christopoulos, A. & Crouch, M. F., 2006, In : Genetic Engineering News. 26, 1, p. 27 - 28 2 p.

Research output: Contribution to journalArticleResearchpeer-review

GPCR allosterism: A novel approach to drug selectivity

Christopoulos, A., 2006, p. 9 - 9. 1 p.

Research output: Contribution to conferenceAbstractOther

1 Citation (Scopus)

G protein-coupled receptor drug targets

Sexton, P. M. & Christopoulos, A., 2006, In : Current Pharmaceutical Design. 12, 14, p. 1681 - 1682 2 p.

Research output: Contribution to journalLetterOther

25 Citations (Scopus)

Interaction studies of multiple binding sites on M4 muscarinic acetylcholine receptors

Lanzafame, A. A., Sexton, P. M. & Christopoulos, A., 2006, In : Molecular Pharmacology. 70, 2, p. 736 - 746 11 p.

Research output: Contribution to journalArticleResearchpeer-review

34 Citations (Scopus)

Mechanisms of ERK1/2 regulation by seven-transmembrane-domain receptors

Werry, T. D., Christopoulos, A. & Sexton, P. M., 2006, In : Current Pharmaceutical Design. 12, 14, p. 1683 - 1702 20 p.

Research output: Contribution to journalArticleResearchpeer-review

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

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

Research output: Contribution to conferenceAbstractOther

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

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

2007
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

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

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

117 Citations (Scopus)

Critical role for the second extracellular loop in the binding of both orthosteric and allosteric G protein-coupled receptor ligands

Avlani, V. A., Gregory, K. J., Morton, C. J., Parker, M. W., Sexton, P. & Christopoulos, A., 2007, In : Journal of Biological Chemistry. 282, 35, p. 25677 - 25686 10 p.

Research output: Contribution to journalArticleResearchpeer-review

81 Citations (Scopus)

Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs

Bisson, W. H., Cheltsov, A. V., Bruey-Sedano, N., Lin, B., Chen, J., Goldberger, N., May, L. T., Christopoulos, A., Dalton, J. T., Sexton, P., Zhang, X-K. & Abagyan, R., 2007, In : Proceedings of the National Academy of Sciences. 104, 29, p. 11927 - 11932 6 p.

Research output: Contribution to journalArticleResearchpeer-review

775 Citations (Scopus)

Functional selectivity and classical concepts of quantitative pharmacology

Urban, J. D., Clarke, W. P., von Zastrow, M., Nichols, D. E., Kobilka, B., Weinstein, H., Javitch, J. A., Roth, B. L., Christopoulos, A., Sexton, P. M., Miller, K. J., Spedding, M. & Mailman, R. B., 2007, In : Journal of Pharmacology and Experimental Therapeutics. 320, 1, p. 1 - 13 13 p.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

History of research on nicotinic and muscarinic cholinergic receptors

Karczmar, A. G., Lindstrom, J. & Christopoulos, A., 2007, Exploring the Vertebrate Central Cholinergic Nervous System. Karczmar, A. G. (ed.). First ed. New York USA: Springer, p. 151 - 162 12 p.

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

21 Citations (Scopus)

Involvement of the sigma1 (sigma1) receptor in the anti-amnesic, but not antidepressant-like, effects of the aminotetrahydrofuran derivative ANAVEX1-41

Espallergues, J., Lapalud, P., Christopoulos, A., Avlani, V. A., Sexton, P., Vamvakides, A. & Maurice, T., 2007, In : British Journal of Pharmacology. 152, 2, p. 267 - 279 13 p.

Research output: Contribution to journalArticleResearchpeer-review

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

94 Citations (Scopus)

Structure-function studies of allosteric agonism at M2 muscarinic acetylcholine receptors

May, L. T., Avlani, V. A., Langmead, C. J., Herdon, H. J., Wood, M. D., Sexton, P. & Christopoulos, A., 2007, In : Molecular Pharmacology. 72, 2, p. 463 - 476 14 p.

Research output: Contribution to journalArticleResearchpeer-review

2008
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

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

129 Citations (Scopus)
16 Citations (Scopus)

Benzodiazepine ligands can act as allosteric modulators of the Type 1 cholecystokinin receptor

Gao, F., Sexton, P., Christopoulos, A. & Miller, L. J., 2008, In : Bioorganic and Medicinal Chemistry Letters. 18, 5, p. 4401 - 4404 4 p.

Research output: Contribution to journalArticleResearchpeer-review

50 Citations (Scopus)

Identification of N-terminal receptor activity-modifying protein residues important for calcitonin gene-related peptide, adrenomedullin, and amylin receptor function

Qi, T., Christopoulos, G., Bailey, R. J., Christopoulos, A., Sexton, P. & Hay, D. L., 2008, In : Molecular Pharmacology. 74, 4, p. 1059 - 1071 13 p.

Research output: Contribution to journalArticleResearchpeer-review