Research Output

2015

Molecular insights into metabotropic glutamate receptor allosteric modulations

Gregory, K. J. & Conn, P. J., 1 Jul 2015, In : Molecular Pharmacology. 88, 1, p. 188-202 15 p.

Research output: Contribution to journalShort SurveyResearchpeer-review

31 Citations (Scopus)

Molecular mechanism of action of triazolobenzodiazepinone agonists of the type 1 cholecystokinin receptor. Possible cooperativity across the receptor homodimeric complex

Desai, A. J., Lam, P. C. H., Orry, A., Abagyan, R., Christopoulos, A., Sexton, P. & Miller, L. J., 2015, In : Journal of Medicinal Chemistry. 58, 24, p. 9562-9577 16 p.

Research output: Contribution to journalArticleResearchpeer-review

10 Citations (Scopus)

Neural regulation of pancreatic cancer: a novel target for intervention

Chang, A., Kim-Fuchs, C., Le, C. P., Hollande, F. & Sloan, E. K., 2015, In : Cancers. 7, 3, p. 1292-1312 21 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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11 Citations (Scopus)

Neuroinflammation and behaviour

Sominsky, L., Walker, A. K. & Hodgson, D. M., 2015, In : Frontiers in Neuroscience. 9, MAY, 3 p., 201.

Research output: Contribution to journalEditorialOtherpeer-review

Open Access
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4 Citations (Scopus)

Neutrophil elastase activates protease-activated receptor-2 (PAR2) and transient receptor potential vanilloid 4 (TRPV4) to cause inflammation and pain

Zhao, P., Lieu, T. M., Barlow, N., Sostegni, S., Haerteis, S., Korbmacher, C., Liedtke, W., Jimenez-Vargas, N. N., Vanner, S. & Bunnett, N. W., 2015, In : The Journal of Biological Chemistry. 290, 22, p. 13875 - 13887 13 p.

Research output: Contribution to journalArticleResearchpeer-review

73 Citations (Scopus)

Novel allosteric modulators of G protein-coupled receptors

Gentry, P. R., Sexton, P. M. & Christopoulos, A., 2015, In : The Journal of Biological Chemistry. 290, 32, p. 19478-19488 11 p.

Research output: Contribution to journalArticleResearchpeer-review

96 Citations (Scopus)

Novel GPCR paradigms at the μ-opioid receptor

Thompson, G. L., Kelly, E., Christopoulos, A. & Canals, M., 2015, In : British Journal of Pharmacology. 172, 2, p. 287-296 10 p.

Research output: Contribution to journalArticleResearchpeer-review

42 Citations (Scopus)

P2Y1 receptor activation of the TRPV4 ion channel enhances purinergic signaling in satellite glial cells

Rajasekhar, P., Poole, D. P., Liedtke, W., Bunnett, N. W. & Veldhuis, N. A., 2015, In : The Journal of Biological Chemistry. 290, 48, p. 29051-29062 12 p.

Research output: Contribution to journalArticleResearchpeer-review

24 Citations (Scopus)

PEGylation does not significantly change the initial intravenous or subcutaneous pharmacokinetics or lymphatic exposure of trastuzumab in rats but increases plasma clearance after subcutaneous administration

Chan, L. J., Bulitta, J. B., Ascher, D. B., Haynes, J. M., McLeod, V. M., Porter, C. J., Williams, C. C. & Kaminskas, L. M., 2015, In : Molecular Pharmaceutics. 12, 3, p. 794 - 809 16 p.

Research output: Contribution to journalArticleResearchpeer-review

17 Citations (Scopus)

Proof of concept study for designed multiple ligands targeting the dopamine D2, serotonin 5-HT2A, and muscarinic M1 acetylcholine receptors

Szabo, M., Lim, H. D., Klein Herenbrink, C., Christopoulos, A., Lane, J. R. D. & Capuano, B., 2015, In : Journal of Medicinal Chemistry. 58, 3, p. 1550 - 1555 6 p.

Research output: Contribution to journalArticleResearchpeer-review

7 Citations (Scopus)

Quantification and potential functions of endogenous agonists of transient receptor potential channels in patients with irritable bowel syndrome

Cenac, N., Bautzova, T., Le Faouder, P., Veldhuis, N. A., Poole, D. P., Rolland, C., Bertrand, J., Liedtke, W., Dubourdeau, M., Bertrand-Michel, J., Zecchi, L., Stanghellini, V., Bunnett, N. W., Barbara, G. & Vergnolle, N., 2015, In : Gastroenterology. 149, 2, p. 433-444 12 p.

Research output: Contribution to journalArticleResearchpeer-review

70 Citations (Scopus)

Quantitative proteome changes in Arabidopsis thaliana suspension-cultured cells in response to plant natriuretic peptides

Turek, I., Wheeler, J. I., Gehring, C., Irving, H. R. & Marondedze, C., 2015, In : Data in Brief. 4, p. 336-343 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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2 Citations (Scopus)

Receptor expression modulates calcium-sensing receptor mediated intracellular Ca2+ mobilization

Brennan, S. C., Mun, H., Leach, K., Kuchel, P. W., Christopoulos, A. & Conigrave, A., 2015, In : Endocrinology. 156, 4, p. 1330 - 1342 13 p.

Research output: Contribution to journalArticleResearchpeer-review

17 Citations (Scopus)

Regulation of RGS5 GAP activity by GPSM3

Zhao, P. & Chidiac, P., 2015, In : Molecular and Cellular Biochemistry. 405, 1-2, p. 33-40 8 p.

Research output: Contribution to journalArticleResearchpeer-review

3 Citations (Scopus)

Role of the astrocytic Na+, K+-ATPase in K+ homeostasis in brain: K+ uptake, signaling pathways and substrate utilization

Hertz, L., Song, D., Xu, J., Peng, L. & Gibbs, M. E., 2015, In : Neurochemical Research. 40, 12, p. 2505-2516 12 p.

Research output: Contribution to journalArticleResearchpeer-review

29 Citations (Scopus)

Sensitisation of TRPV4 by PAR2 is independent of intracellular calcium signalling and can be mediated by the biased agonist neutrophil elastase

Sostegni, S., Diakov, A., McIntyre, P., Bunnett, N., Korbmacher, C. & Haerteis, S., 2015, In : Pflugers Archiv-European Journal of Physiology. 467, 4, p. 687-701 15 p.

Research output: Contribution to journalArticleResearchpeer-review

10 Citations (Scopus)

Serelaxin-mediated signal transduction in human vascular cells: bell-shaped concentration-response curves reflect differential coupling to G proteins

Sarwar, M., Samuel, C. S., Bathgate, R. A., Stewart, D. R. & Summers, R. J., 2015, In : British Journal of Pharmacology. 172, 4, p. 1005-1019 15 p.

Research output: Contribution to journalArticleResearchpeer-review

41 Citations (Scopus)
25 Citations (Scopus)

Synthesis, biological evaluation, and utility of fluorescent ligands targeting the μ-opioid receptor

Schembri, L. S., Stoddart, L. A., Briddon, S. J., Kellam, B., Canals, M., Graham, B. & Scammells, P. J., 2015, In : Journal of Medicinal Chemistry. 58, 24, p. 9754-9767 14 p.

Research output: Contribution to journalArticleResearchpeer-review

11 Citations (Scopus)

Synthesis and pharmacological evaluation of dual acting ligands targeting the adenosine A2A and dopamine D2 receptors for the potential treatment of Parkinson's disease

Jorg, M. T., May, L. T., Mak, F. S., Lee, K. C. K., Miller, N. D., Scammells, P. J. & Capuano, B., 2015, In : Journal of Medicinal Chemistry. 58, 2, p. 718 - 738 21 p.

Research output: Contribution to journalArticleResearchpeer-review

33 Citations (Scopus)

Synthesis and pharmacological evaluation of M4 muscarinic receptor positive allosteric modulators derived from VU10004

Huynh, T., Valant, C., Crosby, I. T., Sexton, P., Christopoulos, A. & Capuano, B., 2015, In : ACS Chemical Neuroscience. 6, 6, p. 838 - 844 7 p.

Research output: Contribution to journalArticleResearchpeer-review

9 Citations (Scopus)

Synthesis of six mexiletine derivatives with isoindolines attached as potential antioxidants and their evaluation as cardioprotective agents

Chau, B. A., Drummond, G. R., Jackson, W. R., Jarrott, B., Miller, A. A., Subasinghe, K. R., Tan, C. Y. R., White, P. J., Wright, C. E. & Ziogas, J., 2015, In : MedChemComm. 6, 4, p. 634-639 6 p.

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)

Tamsulosin modulates, but does not abolish the spontaneous activity in the guinea pig prostate gland

Chakrabarty, B., Dey, A., Lam, M. H-S., Ventura, S. & Exintaris, B., 2015, In : Neurourology and Urodynamics. 34, 5, p. 482-488 7 p.

Research output: Contribution to journalArticleResearchpeer-review

6 Citations (Scopus)

Targeting of transient receptor potential channels in digestive disease

Poole, D. P., Lieu, T., Veldhuis, N. A., Rajasekhar, P. & Bunnett, N. W., 2015, TRP Channels as Therapeutic Targets: From Basic Science to Clinical Use. Szallasi, A. (ed.). London UK: Elsevier, p. 385-403 19 p.

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

1 Citation (Scopus)

The complex roles of mu-opioid receptor phosphorylation: a key determinant in receptor signaling and regulation

Canals, M., 2015, In : Molecular Pharmacology. 88, 4, p. 814 - 815 2 p.

Research output: Contribution to journalLetterOther

3 Citations (Scopus)

The Concise Guide to PHARMACOLOGY 2015/16: Overview

CGTP Collaborators, 1 Dec 2015, In : British Journal of Pharmacology. 172, 24, p. 5729-5743 15 p.

Research output: Contribution to journalReview ArticleOtherpeer-review

Open Access
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153 Citations (Scopus)

The G protein-coupled receptor-transient receptor potential channel axis: molecular insights for targeting disorders of sensation and inflammation

Veldhuis, N. A., Poole, D. P., Grace, M., McIntyre, P. & Bunnett, N. W., 2015, In : Pharmacological Reviews. 67, 1, p. 36 - 73 38 p.

Research output: Contribution to journalArticleResearchpeer-review

71 Citations (Scopus)

The new editorial team

Bunnett, N. W., 5 Aug 2015, In : American Journal of Physiology - Gastrointestinal and Liver Physiology. 309, 3, p. G133-G134

Research output: Contribution to journalEditorialOtherpeer-review

29 Citations (Scopus)

The wiggle index: an open source bioassay to assess sub-lethal insecticide response in Drosophila melanogaster

Denecke, S., Nowell, C. J., Fournier-Level, A., Perry, T. & Batterham, P., 2015, In : PLoS ONE. 10, 12, p. 1-18 18 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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8 Citations (Scopus)

Towards tissue-specific pharmacology: insights from the calcium-sensing receptor as a paradigm for GPCR (patho)physiological bias

Leach, K., Conigrave, A. D., Sexton, P. M. & Christopoulos, A., 2015, In : Trends in Pharmacological Sciences. 36, 4, p. 215-225 11 p.

Research output: Contribution to journalArticleResearchpeer-review

34 Citations (Scopus)

Transient receptor potential vanilloid 4 inhibits mouse colonic motility by activating NO-dependent enteric neurotransmission

Fichna, J., Poole, D. P., Veldhuis, N., MacEachern, S. J., Saur, D., Zakrzewski, P. K., Cygankiewicz, A. I., Mokrowiecka, A., Malecka-Panas, E., Krajewska, W. M., Liedtke, W., Steinhoff, M. S., Timmermans, J-P., Bunnett, N. W., Sharkey, K. A. & Storr, M. A., 2015, In : Journal of Molecular Medicine. 93, 12, p. 1297-1309 13 p.

Research output: Contribution to journalArticleResearchpeer-review

13 Citations (Scopus)

Uptake of the butyrate receptors, GPR41 and GPR43, in lipidic bicontinuous cubic phases suitable for in meso crystallization

Liang, Y-L., Conn, C. E., Drummond, C. J. & Darmanin, C., 2015, In : Journal of Colloid and Interface Science. 441, p. 78 - 84 7 p.

Research output: Contribution to journalArticleResearchpeer-review

7 Citations (Scopus)

Using active learning strategies to shift student attitudes and behaviours about learning and teaching in a research intensive educational context

White, P. J., Larson, I., Styles, K., Yuriev, E., Evans, D. R., Short, J. L., Rangachari, P. K., Malone, D. T., Davie, B., Naidu, S. & Eise, N., 2015, In : Pharmacy Education. 15, 1, p. 116-126 11 p.

Research output: Contribution to journalArticleResearchpeer-review

15 Citations (Scopus)

α2-adrenergic blockade mimics the enhancing effect of chronic stress on breast cancer progression

Lamkin, D. M., Sung, H. Y., Yang, G. S., David, J. M., Ma, J. C. Y., Cole, S. W. & Sloan, E. K., 2015, In : Psychoneuroendocrinology. 51, p. 262-270 9 p.

Research output: Contribution to journalArticleResearchpeer-review

26 Citations (Scopus)

β2-adrenoceptor signaling regulates invadopodia formation to enhance tumor cell invasion

Creed, S. J., Le, C. P., Hassan, M., Pon, C. K., Albold, S., Chan, K. T., Berginski, M. E., Huang, Z., Bear, J. E., Lane, J. R., Halls, M. L., Ferrari, D., Nowell, C. J. & Sloan, E. K., 2015, In : Breast Cancer Research. 17, 1, 12 p., 145.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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34 Citations (Scopus)
2014

Activation of mu opioid receptors sensitizes Transient Receptor Potential Vanilloid Type 1 (TRPV1) via beta-arrestin-2-mediated cross-talk

Rowan, M. P., Bierbower, S. M., Eskander, M. A., Szteyn, K., Por, E. D., Gomez, R., Veldhuis, N. A., Bunnett, N. W. & Jeske, N. A., 2014, In : PLoS ONE. 9, 4, 12 p., e93688.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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28 Citations (Scopus)

Advances in G protein-coupled receptor allostery: From function to structure

Christopoulos, A., 2014, In : Molecular Pharmacology. 86, 5, p. 463 - 478 16 p.

Research output: Contribution to journalArticleResearchpeer-review

124 Citations (Scopus)

Allosteric interactions at adenosine A1 and A3 receptors: New insights into the role of small molecules and receptor dimerization

Hill, S. J., May, L. T., Kellam, B. & Woolard, J., 2014, In : British Journal of Pharmacology. 171, 5, p. 1102 - 1113 12 p.

Research output: Contribution to journalArticleResearchpeer-review

39 Citations (Scopus)

Allosteric modulation of M1 muscarinic acetylcholine receptor internalization and subcellular trafficking

Yeatman, H. R., Lane, J. R. D., Choy, K. H. C., Lambert, N., Sexton, P., Christopoulos, A. & Canals, M., 2014, In : The Journal of Biological Chemistry. 289, 22, p. 15856 - 15866 11 p.

Research output: Contribution to journalArticleResearchpeer-review

19 Citations (Scopus)

Allosteric targeting of receptor tyrosine kinases

De Smet, F., Christopoulos, A. & Carmeliet, P., 2014, In : Nature Biotechnology. 32, 11, p. 1113 - 1120 8 p.

Research output: Contribution to journalArticleResearchpeer-review

40 Citations (Scopus)

A new mechanism of allostery in a G protein-coupled receptor dimer

Lane, J. R. D., Donthamsetti, P., Shonberg, J., Draper-Joyce, C. J., Dentry, S., Michino, M., Shi, L., Lopez Munoz, L., Scammells, P. J., Capuano, B., Sexton, P., Javitch, J. A. & Christopoulos, A., 2014, In : Nature Chemical Biology. 10, 9, p. 745 - 752 8 p.

Research output: Contribution to journalArticleResearchpeer-review

81 Citations (Scopus)

Antagonists of the vasopressin V1 receptor and of the Beta1-adrenoceptor inhibit cytotoxic brain edema in stroke by effects on astrocytes - but the mechanisms differ

Hertz, L., Xu, J., Chen, Y., Gibbs, M. E. & Du, T., 2014, In : Current Neuropharmacology. 12, 4, p. 308 - 323 16 p.

Research output: Contribution to journalArticleResearchpeer-review

17 Citations (Scopus)

A nuclear transport inhibitor that modulates the unfolded protein response and provides in vivo protection against lethal dengue virus infection

Fraser, J. E., Watanabe, S., Wang, C., Chan, W. K. K., Maher, B., Lopez-Denman, A., Hick, C. A., Wagstaff, K. M., Mackenzie, J. M., Sexton, P. M., Vasudevan, S. G. & Jans, D. A., 2014, In : Journal of Infectious Diseases. 210, 11, p. 1780 - 1791 12 p.

Research output: Contribution to journalArticleResearchpeer-review

58 Citations (Scopus)

Application of recombinant technology in protein investigations

Wang, Y. H., Muleya, V. & Irving, H. R., 2014, Protein Purification and Analysis II - Methods and Applications. Hong Kong: iConcept Press, p. 23 - 44 22 p.

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

Biased agonism at G protein-coupled receptors: The promise and the challenges - A medicinal chemistry perspective

Shonberg, J., Lopez Munoz, L., Scammells, P. J., Christopoulos, A., Capuano, B. & Lane, J. R. D., 2014, In : Medicinal Research Reviews. 34, 6, p. 1286 - 1330 45 p.

Research output: Contribution to journalArticleResearchpeer-review

77 Citations (Scopus)

Biased signaling of protease-activated receptors

Zhao, P., Metcalf, M. & Bunnett, N. W., 2014, In : Frontiers in Endocrinology. 5, May 2014, p. 1 - 16 16 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
127 Citations (Scopus)

Binding kinetics differentiates functional antagonism of orexin-2 receptor ligands

Mould, R., Brown, J., Marshall, F. H. & Langmead, C. J., Jan 2014, In : British Journal of Pharmacology. 171, 2, p. 351-363 13 p.

Research output: Contribution to journalArticleResearchpeer-review

49 Citations (Scopus)

Biological redundancy of endogenous GPCR ligands in the gut and the potential for endogenous functional selectivity

Thompson, G. L., Canals, M. & Poole, D. P., 2014, In : Frontiers in Pharmacology. 5, p. 1 - 12 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
18 Citations (Scopus)

Calcium is the switch in the moonlighting dual function of the ligand-activated receptor kinase phytosulfokine receptor 1

Muleya, V., Wheeler, J., Ruzvidzo, O., Freihat, L., Manallack, D. T., Gehring, C. A. & Irving, H. R., 2014, In : Cell Communication and Signaling. 12, p. 1 - 5 5 p., 60.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
27 Citations (Scopus)