1986 …2020

Research output per year

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Article
2010

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

30 Citations (Scopus)
17 Citations (Scopus)

Secretin occupies a single protomer of the homodimeric secretin receptor complex: insights from photoaffinity labeling studies using dual sites of covalent attachment

Dong, M., Lam, P. C-H., Pinon, D. I., Orry, A., Sexton, P., Abagyan, R. & Miller, L. J., 2010, In : The Journal of Biological Chemistry. 285, 13, p. 9919 - 9931 13 p.

Research output: Contribution to journalArticleResearchpeer-review

19 Citations (Scopus)
52 Citations (Scopus)

The effect of social isolation on rat brain expression of genes associated with endocannabinoid signaling

Robinson, S. A., Loiacono, R., Christopoulos, A., Sexton, P. & Malone, D. T., 2010, In : Brain Research. 1343, p. 153 - 167 15 p.

Research output: Contribution to journalArticleResearchpeer-review

38 Citations (Scopus)
2009

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

28 Citations (Scopus)
94 Citations (Scopus)

Functional importance of a structurally distinct homodimeric complex of the family B G protein-coupled secretin receptor

Gao, F., Harikumar, K. G., Dong, M., Lam, P. C-H., Sexton, P. M., Christopoulos, A., Bordner, A., Abagyan, R. & Miller, L. J., 2009, In : Molecular Pharmacology. 76, 2, p. 264 - 274 11 p.

Research output: Contribution to journalArticleResearchpeer-review

43 Citations (Scopus)

Modulating receptor function through RAMPs: can they represent drug targets in themselves?

Sexton, P. M., Poyner, D. R., Simms, J. W., Christopoulos, A. & Hay, D. L., 2009, In : Drug Discovery Today. 14, 7-8, p. 413 - 419 7 p.

Research output: Contribution to journalArticleResearchpeer-review

53 Citations (Scopus)

Molecular basis of association of receptor activity-modifying protein 3 with the family B G protein-coupled secretin receptor

Harikumar, K. G., Simms, J., Christopoulos, G., Sexton, P. M. & Miller, L. J., 15 Dec 2009, In : Biochemistry. 48, 49, p. 11773-11785 13 p.

Research output: Contribution to journalArticleResearchpeer-review

38 Citations (Scopus)
2008

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

39 Citations (Scopus)
132 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

16 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

53 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

87 Citations (Scopus)

Pattern of Intra-Family Hetero-Oligomerization Involving the G-Protein-Coupled Secretin Receptor

Harikumar, K. G., Morfis, M., Sexton, P. & Miller, L. J., 2008, In : Journal of Molecular Neuroscience. 36, 1-3, p. 279 - 285 7 p.

Research output: Contribution to journalArticleResearchpeer-review

42 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

15 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

34 Citations (Scopus)

Receptor activity-modifying proteins differentially modulate the G protein-coupling efficiency of amylin receptors

Morfis, M., Tilakaratne, N., Furness, S. G. B., Christopoulos, G., Werry, T. D., Christopoulos, A. & Sexton, P., 2008, In : Endocrinology. 149, 11, p. 5423 - 5431 9 p.

Research output: Contribution to journalArticleResearchpeer-review

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80 Citations (Scopus)

RNA editing of the serotonin 5HT2C receptor and its effects on cell signalling, pharmacology and brain function

Werry, T. D., Loiacono, R., Sexton, P. & Christopoulos, A., 2008, In : Pharmacology and Therapeutics. 119, 1, p. 7 - 23 17 p.

Research output: Contribution to journalArticleResearchpeer-review

115 Citations (Scopus)

Spatial approximation between secretin residue five and the third extracellular loop of its receptor provides new insight into the molecular basis of natural agonist binding

Dong, M., Lam, P. C-H., Pinon, D. I., Sexton, P., Abagyan, R. & Miller, L. J., 2008, In : Molecular Pharmacology. 74, 2, p. 413 - 422 10 p.

Research output: Contribution to journalArticleResearchpeer-review

31 Citations (Scopus)

The effects of C-terminal truncation of receptor activity modifying proteins on the induction of amylin receptor phenotype from human CTb receptors

Udawela, M., Christopoulos, G., Morfis, M., Tilakaratne, N., Christopoulos, A. & Sexton, P., 2008, In : Regulatory Peptides. 145, p. 65 - 71 6 p.

Research output: Contribution to journalArticleResearchpeer-review

11 Citations (Scopus)

The impact of orthosteric radioligand depletion on the quantification of allosteric modulator interactions

Avlani, V. A., McLoughlin, D. J., Sexton, P. & Christopoulos, A., 2008, In : Journal of Pharmacology and Experimental Therapeutics. 325, 3, p. 927 - 934 8 p.

Research output: Contribution to journalArticleResearchpeer-review

9 Citations (Scopus)
2007

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

258 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

500 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

78 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 : The Journal of Biological Chemistry. 282, 35, p. 25677 - 25686 10 p.

Research output: Contribution to journalArticleResearchpeer-review

120 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 of the United States of America. 104, 29, p. 11927 - 11932 6 p.

Research output: Contribution to journalArticleResearchpeer-review

81 Citations (Scopus)

Fluorescence resonance energy transfer analysis of secretin docking to its receptor: Mapping distances between residues distributed throughout the ligand pharmacophore and distinct receptor residues

Harikumar, K. G., Lam, P. C-H., Dong, M., Sexton, P., Abagyan, R. & Miller, L. J., 2007, In : The Journal of Biological Chemistry. 282, 45, p. 32834 - 32843 10 p.

Research output: Contribution to journalArticleResearchpeer-review

25 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

803 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

21 Citations (Scopus)

Molecular approximations between residues 21 and 23 of secretin and its receptor: Development of a model for peptide docking with the amino terminus of the secretin receptor

Dong, M., Lam, P. C-H., Gao, F., Hosohata, K., Pinon, D. I., Sexton, P., Abagyan, R. & Miller, L. J., 2007, In : Molecular Pharmacology. 72, 2, p. 280 - 290 11 p.

Research output: Contribution to journalArticleResearchpeer-review

30 Citations (Scopus)

Relaxin receptors - new drug targets for multiple disease states

van der Westhuizen, E. T., Summers, R. J., Halls, M. L., Bathgate, R. & Sexton, P., 2007, In : Current Drug Targets. 8, 1, p. 91 - 104 14 p.

Research output: Contribution to journalArticleResearchpeer-review

21 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

94 Citations (Scopus)

The relaxin family peptide receptor 3 activates extracellular signal-regulated kinase 1/2 through a protein kinase C-dependent mechanism

van der Westhuizen, E. T., Werry, T. D., Sexton, P. & Summers, R. J., 2007, In : Molecular Pharmacology. 71, 6, p. 1618 - 1629 12 p.

Research output: Contribution to journalArticleResearchpeer-review

64 Citations (Scopus)
2006

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

31 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

73 Citations (Scopus)

Constitutive formation of oligomeric complexes between family B G protein-coupled vasoactive intestinal polypeptide and secretin receptors

Harikumar, K. G., Morfis, M. M., Lisenbee, C. S., Sexton, P. M. & Miller, L. J., 2006, In : Molecular Pharmacology. 69, 1, p. 363 - 373 11 p.

Research output: Contribution to journalArticleResearchpeer-review

54 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

43 Citations (Scopus)

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 modulation by RAMPs

Hay, D. L., Poyner, D. R. & Sexton, P. M., 2006, In : Pharmacology and Therapeutics. 109, 1-2, p. 173 - 197 25 p.

Research output: Contribution to journalArticleResearchpeer-review

200 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

25 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

34 Citations (Scopus)
2005

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

70 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

9 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

274 Citations (Scopus)

G-Protein-coupled receptor-protein interactions: basis for new concepts on receptor structure and function

Tilakaratne, N. & Sexton, P. M., 2005, In : Clinical and Experimental Pharmacology and Physiology. 32, 11, p. 979 - 987 9 p.

Research output: Contribution to journalArticleResearchpeer-review

29 Citations (Scopus)