Research Output

2012

Ramp

Hay, D. L., Sexton, P. M. & Poyner, D. R., 2012, Encyclopedia of Signaling Molecules. Choi, S. (ed.). New York NY USA: Springer, p. 1570-1574 5 p.

Research output: Chapter in Book/Report/Conference proceedingEncyclopaedia / Dictionary EntryOtherpeer-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

10 Citations (Scopus)

Rapid turnover of glycogen in memory formation

Gibbs, M. E. & Hutchinson, D. S., 2012, In : Neurochemical Research. 37, 11, p. 2456 - 2463 8 p.

Research output: Contribution to journalArticleResearchpeer-review

24 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 : The Journal of Biological Chemistry. 287, 6, p. 3659 - 3673 15 p.

Research output: Contribution to journalArticleResearchpeer-review

22 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 : The Journal of Biological Chemistry. 287, 6, p. 3642 - 3658 17 p.

Research output: Contribution to journalArticleResearchpeer-review

64 Citations (Scopus)

Sequential conformational rearrangements dictate the dynamics of class C GPCR activation

Lane, J. R. D. & Canals, M., 2012, In : Science Signaling. 5, 251, p. 1 - 3 3 p.

Research output: Contribution to journalLetterOther

2 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

37 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 : The Journal of Biological Chemistry. 287, 44, p. 37066 - 37077 12 p.

Research output: Contribution to journalArticleResearchpeer-review

24 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

13 Citations (Scopus)

Suppressing production of reactive oxygen species (ROS) for influenza A virus therapy

Vlahos, R., Stambas, J. & Selemidis, S., 2012, In : Trends in Pharmacological Sciences. 33, 1, p. 3 - 8 6 p.

Research output: Contribution to journalArticleResearchpeer-review

83 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

39 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

5 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

118 Citations (Scopus)

The expression of calcitonin receptor detected in malignant cells of the brain tumour glioblastoma multiforme and functional properties in the cell line A172

Wookey, P. J., McLean, C. A., Hwang, P. Y. K., Furness, S. G. B., Nguyen, S., Kourakis, A., Hare, D. L. & Rosenfeld, J. V., 2012, In : Histopathology. 60, 6, p. 895 - 910 16 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
12 Citations (Scopus)

The involvement of a Na+ - and Cl- -dependent transporter in the brain uptake of amantadine and rimantadine

Kooijmans, S. A. A., Senyschyn, D., Mezhiselvam, M. M., Morizzi, J., Charman, S. A., Weksler, B., Romero, I-A., Couraud, P. & Nicolazzo, J., 2012, In : Molecular Pharmaceutics. 9, p. 883 - 893 11 p.

Research output: Contribution to journalArticleResearchpeer-review

14 Citations (Scopus)

Themed section: Molecular Pharmacology of G protein-coupled receptors

Summers, R., 2012, In : British Journal of Pharmacology. 165, 6, p. 1609 - 1612 4 p.

Research output: Contribution to journalLetterOther

1 Citation (Scopus)

Toward the establishment of standardized in vitro tests for lipid-based formulations, Part 1: Method parameterization and comparison of in vitro digestion profiles across a range of representative formulations

Williams, H. D., Sassene, P. J., Kleberg, K., Bakala-N'Goma, J-C., Calderone, M., Jannin, V., Igonin, A., Partheil, A., Marchaud, D., Jule, E., Vertommen, J., Maio, M., Blundell, R., Benameur, H., Carriere, F., Mullertz, A., Porter, C. J. & Pouton, C. W., 2012, In : Journal of Pharmaceutical Sciences. 101, 9, p. 3360 - 3380 21 p.

Research output: Contribution to journalArticleResearchpeer-review

156 Citations (Scopus)

Xenobiotics and loss of cell adhesion drive distinct transcriptional outcomes by aryl hydrocarbon receptor signaling

Hao, N., Lee, K. L., Furness, S. G. B., Bosdotter, C., Poellinger, L. & Whitelaw, M. L., 2012, In : Molecular Pharmacology. 82, 6, p. 1082 - 1093 12 p.

Research output: Contribution to journalArticleResearchpeer-review

20 Citations (Scopus)
2011

Agonist activation of the G protein-coupled receptor GPR35 involves transmembrane domain III and is transduced via Galpha13 and beta-arrestin-2

Jenkins, L., Alvarez-Curto, E., Campbell, K., de Munnik, S., Canals, M., Schlyer, S. & Milligan, G., 2011, In : British Journal of Pharmacology. 162, 3, p. 733 - 748 16 p.

Research output: Contribution to journalArticleResearchpeer-review

41 Citations (Scopus)

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

207 Citations (Scopus)

Allosteric modulation of metabotropic glutamate receptors

Sheffler, D. J., Gregory, K. J., Rook, J. M. & Conn, P. J., 2011, In : Advances in Pharmacology. 62, p. 37 - 77 41 p.

Research output: Contribution to journalArticleResearchpeer-review

46 Citations (Scopus)

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 : The Journal of Biological Chemistry. 286, 11, p. 8786 - 8797 12 p.

Research output: Contribution to journalArticleResearchpeer-review

54 Citations (Scopus)

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

51 Citations (Scopus)

alpha{2}-Adrenoceptors activate noradrenaline-mediated glycogen turnover in chick astrocytes

Hutchinson, D. S., Catus, S. L., Merlin, J., Summers, R. J. & Gibbs, M. E., 2011, In : Journal of Neurochemistry. 117, 5, p. 915 - 926 12 p.

Research output: Contribution to journalArticleResearchpeer-review

21 Citations (Scopus)

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

26 Citations (Scopus)

Application of G protein-coupled receptor-heteromer identification technology to monitor beta-arrestin recruitment to G protein-coupled receptor heteromers

See, H. B., Seeber, R. M., Kocan, M., Eidne, K. A. & Pfleger, K. D. G., 2011, In : Assay and Drug Development Technologies. 9, 1, p. 21 - 30 10 p.

Research output: Contribution to journalArticleResearchpeer-review

39 Citations (Scopus)

Applications for Activity-based Probes in Drug Discovery

Edgington, L. E. & Bogyo, M., 2011, New Frontiers in Chemical Biology: Enabling Drug Discovery. Bunnage, M. E. (ed.). Cambridge UK: The Royal Society of Chemistry, p. 33-63 31 p. (RSC Drug Discovery Series; no. 5).

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

ATP derived from astrocytes modulates memory in the chick

Gibbs, M. E., Shleper, M., Mustafa, T., Burnstock, G. & Bowser, D. N., 2011, In : Neuron Glia Biology. 7, 2-4, p. 177 - 186 10 p.

Research output: Contribution to journalArticleResearchpeer-review

9 Citations (Scopus)

Cathepsin s is activated during colitis and causes visceral hyperalgesia by a PAR(2)-dependent mechanism in mice

Cattaruzza, F., Lyo, V., Jones, E., Pham, D., Hawkins, J., Kirkwood, K., Valdez-Morales, E., Ibeakanma, C., Vanner, S., Bogyo, M. & Bunnett, N., 2011, In : Gastroenterology. 141, 5, p. 1864 - 1874 11 p.

Research output: Contribution to journalArticleResearchpeer-review

57 Citations (Scopus)

CGRP induction in cystic fibrosis airways alters the submucosal gland progenitor cell niche in mice

Xie, W., Fisher, J., Lynch, T., Luo, M., Evans, T., Neff, T., Zhou, W., Zhang, Y., Ou, Y., Bunnett, N., Russo, A., Goodheart, M., Parekh, K., Liu, X. & Engelhardt, J., 2011, In : Journal of Clinical Investigation. 121, 8, p. 3144 - 3158 15 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
25 Citations (Scopus)

Enhanced BRET technology for the monitoring of agonist-induced and agonist-independent interactions between GPCRs and beta-arrestins

Kocan, M., Dalrymple, M. B., Seeber, R., Feldman, B. J. & Pfleger, K., 2011, In : Frontiers in Endocrinology. 1, p. 1 - 9 9 p., 12.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
15 Citations (Scopus)

Evolution of beta-blockers: from anti-anginal drugs to ligand-directed signalling

Baker, J. G., Hill, S. J. & Summers, R. J., 2011, In : Trends in Pharmacological Sciences. 32, 4, p. 227 - 234 8 p.

Research output: Contribution to journalArticleResearchpeer-review

76 Citations (Scopus)

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

44 Citations (Scopus)

Inhibition of nox2 oxidase activity ameliorates influenza a virus-induced lung inflammation

Vlahos, R., Stambas, J., Bozinovski, S., Broughton, B. RS., Drummond, G. R. & Selemidis, S., 2011, In : PLoS Pathogens. 7, 2, p. 1 - 12 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
143 Citations (Scopus)

Insulin-like peptide 5 (INSL5)

Van Der Westhuizen, E. T., 2011, xPharm: The Comprehensive Pharmacology Reference. Enna, S. J. & Bylund, D. B. (eds.). Elsevier, p. 1-4 4 p.

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

53 Citations (Scopus)

Localization and regulation of fluorescently labeled delta opioid receptor, expressed in enteric neurons of mice

Poole, D., Pelayo, J-C., Scherrer, G., Evans, C., Kieffer, B. & Bunnett, N., 2011, In : Gastroenterology. 141, 3, p. 982 - 991 10 p.

Research output: Contribution to journalArticleResearchpeer-review

42 Citations (Scopus)

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

50 Citations (Scopus)

Molecular basis of secretin docking to its intact receptor using multiple photolabile probes distributed throughout the

Dong, M., Lam, P., Pinon, D., Orry, A., Sexton, P., Abagyan, R. & Miller, L. J., 2011, In : The Journal of Biological Chemistry. 286, 27, p. 23888 - 23899 12 p.

Research output: Contribution to journalArticleResearchpeer-review

24 Citations (Scopus)

Plant natriuretic peptides: control of synthesis and systemic effects

Wang, Y. H., Donaldson, L., Gehring, C. & Irving, H. R., Oct 2011, In : Plant Signaling and Behavior. 6, 10, p. 1606-1608 3 p.

Research output: Contribution to journalArticleOtherpeer-review

5 Citations (Scopus)

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

54 Citations (Scopus)

Protein phosphatase 2A mediates resensitization of the neurokinin 1 receptor

Murphy, J., Roosterman, D., Cottrell, G., Padilla, B., Feld, M., Brand, E., Cedron, W., Bunnett, N. & Steinhoff, M., 2011, In : American Journal of Physiology - Cell Physiology. 301, 4, p. 780 - 791 12 p.

Research output: Contribution to journalArticleResearchpeer-review

16 Citations (Scopus)

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

13 Citations (Scopus)

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

54 Citations (Scopus)

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

Refinement of glucagon-like peptide 1 docking to its intact receptor using mid-region photolabile probes and molecular modeling

Miller, L. J., Chen, Q., Lam, P. C-H., Pinon, D. I., Sexton, P., Abagyan, R. & Dong, M., 2011, In : The Journal of Biological Chemistry. 286, 18, p. 15895 - 15907 13 p.

Research output: Contribution to journalArticleResearchpeer-review

50 Citations (Scopus)

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

179 Citations (Scopus)

Role of beta-adrenoceptors in glucose uptake in astrocytes using beta-adrenoceptor knockout mice

Catus, S. L., Gibbs, M. E., Sato, M., Summers, R. J. & Hutchinson, D. S., 2011, In : British Journal of Pharmacology. 162, 8, p. 1700 - 1715 16 p.

Research output: Contribution to journalArticleResearchpeer-review

33 Citations (Scopus)

Serine proteases mediate inflammatory pain in acute pancreatitis

Ceppa, E., Lyo, V., Grady, E., Knecht, W., Grahn, S., Peterson, A., Bunnett, N., Kirkwood, K. & Cattaruzza, F., 2011, In : American Journal of Physiology - Gastrointestinal and Liver Physiology. 300, p. 1033 - 1042 10 p.

Research output: Contribution to journalArticleResearchpeer-review

22 Citations (Scopus)

Shikonin increases glucose uptake in skeletal muscle cells and improves plasma glucose levels in diabetic goto-kakizaki rats

Oberg, A., Yassin, K., Csikasz, R., Dehvari, N., Shabalina, I., Hutchinson, D., Wilcke, M., Goran-Ostenson, C. & Bengtsson, T., 2011, In : PLoS ONE. 6, 7, 10 p., e22510.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
23 Citations (Scopus)