Research Output

2010

Molecular pharmacology of G protein-coupled receptors: Editorial

Summers, R., 2010, In : British Journal of Pharmacology. 159, 5, p. 983 - 985 3 p.

Research output: Contribution to journalArticleResearchpeer-review

4 Citations (Scopus)

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

32 Citations (Scopus)

Pungent general anesthetics activate transient receptor potential-A1 to produce hyperalgesia and neurogenic bronchoconstriction

Eilers, H., Cattaruzza, F., Nassini, R., Materazzi, S., Andre, E., Chu, C., Cottrell, G., Schumacher, M., Geppetti, P. & Bunnett, N., 2010, In : Anesthesiology. 112, 6, p. 1452 - 1463 12 p.

Research output: Contribution to journalArticleResearchpeer-review

46 Citations (Scopus)

Second Messenger Assays for G Protein-Coupled Receptors: cAMP, Ca2+, Inositol Phosphates, ERK1/2

Gregory, K. J., Sexton, P. M., Christopoulos, A. & Hick, C. A., 25 Jan 2010, G Protein-Coupled Receptors: Essential Methods. Wiley-Blackwell, p. 31-52 22 p.

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

1 Citation (Scopus)

Structure-based discovery of novel chemotypes for adenosine A2A receptor antagonists

Katritch, V., Jaakola, V-P., Lane, J., Lin, J., IJzerman, A. P., Yeager, M., Kufareva, I., Stevens, R. & Abagyan, R., 2010, In : Journal of Medicinal Chemistry. 53, 4, p. 1799 - 1809 11 p.

Research output: Contribution to journalArticleResearchpeer-review

198 Citations (Scopus)

Sub-picomolar relaxin signalling by a pre-assembled RXFP1, AKAP79, AC2, beta-arrestin 2, PDE4D3 complex

Halls, M. & Cooper, D., 2010, In : The EMBO Journal. 29, 16, p. 2772 - 2787 16 p.

Research output: Contribution to journalArticleResearchpeer-review

52 Citations (Scopus)

The Emergence of Allosteric Modulators for G Protein-Coupled Receptors

Gregory, K. J., Valant, C., Simms, J., Sexton, P. M. & Christopoulos, A., 15 Jul 2010, GPCR Molecular Pharmacology and Drug Targeting: Shifting Paradigms and New Directions. John Wiley & Sons, p. 61-87 27 p.

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

4 Citations (Scopus)

The endocannabinoid 2-arachidonylglycerol is a negative allosteric modulator of the human A3 adenosine receptor

Lane, J., Beukers, M., Mulder-Krieger, T. & IJzerman, A. P., 2010, In : Biochemical Pharmacology. 79, 1, p. 48 - 56 9 p.

Research output: Contribution to journalArticleResearchpeer-review

29 Citations (Scopus)

Tissue functions mediated by beta3-adrenoceptors-Findings and challenges

Michel, M., Ochodnicky, P. & Summers, R., 2010, In : Naunyn-Schmiedeberg's Archives of Pharmacology. 382, 2, p. 103 - 108 6 p.

Research output: Contribution to journalArticleResearchpeer-review

27 Citations (Scopus)

Trafficking and signaling of G protein-coupled receptors in the nervous system: implications for disease and therapy

Bunnett, N. & Cottrell, G., 2010, In : CNS and Neurological Disorders - Drug Targets. 9, 5, p. 539 - 556 18 p.

Research output: Contribution to journalArticleResearchpeer-review

13 Citations (Scopus)

Transient receptor potential ankyrin-1 has a major role in mediating visceral pain in mice

Cattaruzza, F., Spreadbury, I., Miranda-Morales, M., Grady, E., Vanner, S. & Bunnett, N., 2010, In : American Journal of Physiology - Gastrointestinal and Liver Physiology. 298, p. 81 - 91 11 p.

Research output: Contribution to journalArticleResearchpeer-review

91 Citations (Scopus)

Transient receptor potential ion channels V4 and A1 contribute to pancreatitis pain in mice

Ceppa, E., Cattaruzza, F., Lyo, V., Amadesi, S., Pelayo, J-C., Poole, D., Vaksman, N., Liedtke, W., Cohen, D., Grady, E., Bunnett, N. & Kirkwood, K., 2010, In : American Journal of Physiology - Gastrointestinal and Liver Physiology. 299, p. 556 - 571 16 p.

Research output: Contribution to journalArticleResearchpeer-review

64 Citations (Scopus)

Understanding amylin Receptors

Just, R., Simms, J., Furness, S. G. B., Christopoulos, A. & Sexton, P. M., 2010, The Calcitonin Gene-related Peptide Family: Form, Function and Future Perspectives. Springer, p. 41-57 17 p.

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

2 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

53 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

50 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
142 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

49 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

4 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

53 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)

Status of GPCR modeling and docking as reflected by community-wide GPCR Dock 2010 assessment

Kufareva, I., Rueda, M., Katritch, V., Stevens, R. C., Abagyan, R., McRobb, F. M., Capuano, B., Crosby, I. T., Chalmers, D. K., Yuriev, E., Simms, J. W., Sexton, P., Wootten, D. L. & Hall, N. E., 2011, In : Structure. 19, 8, p. 1108 - 1126 19 p.

Research output: Contribution to journalArticleResearchpeer-review

229 Citations (Scopus)

Structure activity relationships of trans-substituted-propenoic acid derivatives on the nicotinic acid receptor HCA2 (GPR109A)

van Veldhoven, J. P. D., Blad, C. C., Artsen, C. M., Klopman, C., Wolfram, D. R., Abdelkadir, M. J., Lane, J., Brussee, J. & IJzerman, A. P., 2011, In : Bioorganic and Medicinal Chemistry Letters. 21, 9, p. 2736 - 2739 4 p.

Research output: Contribution to journalArticleResearchpeer-review

8 Citations (Scopus)

Structure-function analysis of amino acid 74 of human RAMP1 and RAMP3 and its role in peptide interactions with adrenomedullin and calcitonin gene-related peptide receptors

Qi, T., Ly, K., Poyner, D. R., Christopoulos, G., Sexton, P. & Hay, D. L., 2011, In : Peptides. 32, 5, p. 1060 - 1067 8 p.

Research output: Contribution to journalArticleResearchpeer-review

20 Citations (Scopus)

The role of placental homeobox genes in human fetal growth restriction

Murthi, P., Rajaraman, G., Brennecke, S. P. & Kalionis, B., 2011, In : Journal of Pregnancy. 2011, 11 p., 548171.

Research output: Contribution to journalReview ArticleResearchpeer-review

Open Access
8 Citations (Scopus)