1986 …2023
If you made any changes in Pure these will be visible here soon.

Research Output 1986 2019

Filter
Article
2009
27 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

90 Citations (Scopus)
42 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

53 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

36 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

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

131 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

53 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

85 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

41 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

15 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

34 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

75 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

Open Access
File
112 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

31 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

10 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

9 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

2007
249 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

490 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

77 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

120 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

25 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 : Journal of Biological Chemistry. 282, 45, p. 32834 - 32843 10 p.

Research output: Contribution to journalArticleResearchpeer-review

785 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

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

30 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

19 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

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

63 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

2006
30 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

70 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

54 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

43 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

197 Citations (Scopus)

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

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

2005
70 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

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

272 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

29 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

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

25 Citations (Scopus)

Insights into interactions between the alpha-helical region of the salmon calcitonin antagonists and the human calcitonin receptor using photoaffinity labeling

Pham, V., Dong, M., Wade, J. D., Miller, L. J., Morton, C. J., Ng, H., Parker, M. W. & Sexton, P. M., 2005, In : Journal of Biological Chemistry. 280, 31, p. 28610 - 28622 13 p.

Research output: Contribution to journalArticleResearchpeer-review

13 Citations (Scopus)

Peptide-oligonucleotide hybrids in antisense therapy

Pierce, T. L., White, A. R., Tregear, G. W. & Sexton, P. M., 2005, In : Mini reviews in medicinal chemistry. 5, 1, p. 41 - 55 15 p.

Research output: Contribution to journalArticleResearchpeer-review

132 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)