Research Output

2016

Macromolecular hydrogen sulfide donors trigger spatiotemporally confined changes in cell signaling

Ercole, F., Mansfeld, F. M., Kavallaris, M., Whittaker, M. R., Quinn, J. F., Halls, M. L. & Davis, T. P., 11 Jan 2016, In : Biomacromolecules. 17, 1, p. 371-383 13 p.

Research output: Contribution to journalArticleResearchpeer-review

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21 Citations (Scopus)

Metabolomics and lipidomics reveal perturbation of sphingolipid metabolism by a novel anti-trypanosomal 3-(oxazolo[4,5-b]pyridine-2-yl)anilide

Stoessel, D., Nowell, C. J., Jones, A. J., Ferrins, L., Ellis, K. M., Riley, J., Rahmani, R., Read, K. D., McConville, M. J., Avery, V. M., Baell, J. B. & Creek, D. J., 1 Jul 2016, In : Metabolomics. 12, 7, 14 p., 126.

Research output: Contribution to journalArticleResearchpeer-review

10 Citations (Scopus)

Metabotropic glutamate receptor subtype 5: molecular pharmacology, allosteric modulation and stimulus bias

Sengmany, K. & Gregory, K. J., 1 Oct 2016, In : British Journal of Pharmacology. 173, 20, p. 3001-3017 17 p.

Research output: Contribution to journalArticleResearchpeer-review

23 Citations (Scopus)

Microglial activation and progressive brain changes in schizophrenia

Laskaris, L., Di Biase, M. A., Everall, I. P., Chana, G., Christopoulos, A., Skafidas, E. S., Cropley, V. L. & Pantelis, C., 2016, In : British Journal of Pharmacology. 173, 4, p. 666-680 15 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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81 Citations (Scopus)

Molecular mechanisms of action of M5 muscarinic acetylcholine receptor allosteric modulators

Berizzi, A. E., Gentry, P. R., Rueda, P., Hoedt, S. D., Sexton, P. M., Langmead, C. J. & Christopoulos, A., 1 Oct 2016, In : Molecular Pharmacology. 90, 4, p. 427-436 10 p.

Research output: Contribution to journalArticleResearchpeer-review

12 Citations (Scopus)

Molecular pharmacology of G protein-coupled receptors

Summers, R. J., 1 Oct 2016, In : British Journal of Pharmacology. 173, 20, p. 2931-2933 3 p.

Research output: Contribution to journalEditorialOtherpeer-review

1 Citation (Scopus)

Monotreme glucagon-like peptide-1 in venom and gut: one gene - two very different functions

Tsend-Ayush, E., He, C., Myers, M. A., Andrikopoulos, S., Wong, N., Sexton, P. M., Wootten, D., Forbes, B. E. & Grutzner, F., 29 Nov 2016, In : Scientific Reports. 6, 12 p., 37744.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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5 Citations (Scopus)

Multivalent approaches and beyond: novel tools for the investigation of dopamine D2 receptor pharmacology

Kopinathan, A., Scammells, P. J., Lane, J. R. & Capuano, B., 1 Jul 2016, In : Future Medicinal Chemistry. 8, 11, p. 1349-1372 24 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

3 Citations (Scopus)

Murine GPRC6A mediates cellular responses to L-amino acids, but not osteocalcin variants

Rueda, P., Harley, E., Lu, Y., Stewart, G. D., Fabb, S., Diepenhorst, N., Cremers, B., Rouillon, M-H., Wehrle, I., Geant, A., Lamarche, G., Leach, K., Charman, W. N., Christopoulos, A., Summers, R. J., Sexton, P. M. & Langmead, C. J., 1 Jan 2016, In : PLoS ONE. 11, 1, p. 1-19 19 p., e0146846.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
27 Citations (Scopus)

Neural regulation of cancer: From mechanobiology to inflammation

Kim, T. H., Rowat, A. C. & Sloan, E. K., 13 May 2016, In : Clinical & Translational Immunology. 5, 9 p., e78.

Research output: Contribution to journalReview ArticleResearchpeer-review

Open Access
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12 Citations (Scopus)

Neurotensin-induced miR-133α expression regulates neurotensin receptor 1 recycling through its downstream target aftiphilin

Law, I. K. M., Jensen, D., Bunnett, N. W. & Pothoulakis, C., 23 Feb 2016, In : Scientific Reports. 6, 14 p., 22195.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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2 Citations (Scopus)

Novel fused arylpyrimidinone based allosteric modulators of the M1 muscarinic acetylcholine receptor

Mistry, S. N., Lim, H., Jorg, M., Capuano, B., Christopoulos, A., Lane, J. R. & Scammells, P. J., 18 May 2016, In : ACS Chemical Neuroscience. 7, 5, p. 647-661 15 p.

Research output: Contribution to journalArticleResearchpeer-review

9 Citations (Scopus)

Novel irreversible agonists acting at the A1 adenosine receptor

Jorg, M., Glukhova, A., Abdul Ridha, A., Vecchio, E. A., Nguyen, A., Sexton, P., White, P., May, L., Christopoulos, A. & Scammells, P., 22 Dec 2016, In : Journal of Medicinal Chemistry. 59, 24, p. 11182-11194 13 p.

Research output: Contribution to journalArticleResearchpeer-review

9 Citations (Scopus)

Optimized method for untargeted metabolomics analysis of MDA-MB-231 breast cancer cells

Peterson, A. L., Walker, A. K., Sloan, E. K. & Creek, D. J., 1 Dec 2016, In : Metabolites. 6, 4, 16 p., 30.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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5 Citations (Scopus)

Orthosteric, allosteric and biased signalling at the relaxin-3 receptor RXFP3

Kocan, M., Ang, S. Y. & Summers, R. J., 2016, In : Neurochemical Research. 41, 3, p. 610-619 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Passive tumour targeting and extravasation of cylindrical polymer brushes in mouse xenografts

Mullner, M., Mehta, D., Nowell, C. & Porter, C. J., Mar 2016, In : Chemical Communications. 52, 58, p. 9121-9124 4 p.

Research output: Contribution to journalArticleOtherpeer-review

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16 Citations (Scopus)

Pathophysiological roles of proteases in gastrointestinal disease

Edgington-Mitchell, L. E., 15 Feb 2016, In : American Journal of Physiology - Gastrointestinal and Liver Physiology. 310, 4, p. G234-G239 6 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

10 Citations (Scopus)

Phosphorylation of the dimeric cytoplasmic domain of the phytosulfokine receptor, PSKR1

Muleya, V., Marondedze, C., Wheeler, J. I., Thomas, L., Mok, Y. F., Griffin, M. D. W., Manallack, D. T., Kwezi, L., Lilley, K. S., Gehring, C. & Irving, H. R., 2016, In : Biochemical Journal. 473, 19, p. 3081-3098 18 p.

Research output: Contribution to journalArticleResearchpeer-review

8 Citations (Scopus)

Plasma membrane localization of the μ-opioid receptor controls spatiotemporal signaling

Halls, M., Yeatman, H. R., Nowell, C. J., Thompson, G. L., Gondin, A. B., Civciristov, S., Bunnett, N. W., Lambert, N. A., Poole, D. P. & Canals, M., 9 Feb 2016, In : Science Signaling. 9, 414, p. 1-13 13 p., ra16.

Research output: Contribution to journalArticleResearchpeer-review

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42 Citations (Scopus)
Open Access
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9 Citations (Scopus)

Practical and low cost whole-organism motility assay: a step-by-step protocol

Preston, S., Jabbar, A., Nowell, C., Joachim, A., Ruttkowski, B., Cardno, T., Hofmann, A. & Gasser, R. B., 1 Feb 2016, In : Molecular and Cellular Probes. 30, 1, p. 13-17 5 p.

Research output: Contribution to journalArticleOtherpeer-review

19 Citations (Scopus)

Practical strategies and concepts in GPCR allosteric modulator discovery: recent advances with metabotropic glutamate receptors

Lindsley, C. W., Emmitte, K. A., Hopkins, C. R., Bridges, T. M., Gregory, K. J., Niswender, C. M. & Conn, P. J., 8 Jun 2016, In : Chemical Reviews. 116, 11, p. 6707-6741 35 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

100 Citations (Scopus)

Prediction of loops in G protein-coupled receptor homology models: effect of imprecise surroundings and constraints

Arora, B., Coudrat, T., Wootten, D., Christopoulos, A., Noronha, S. B. & Sexton, P. M., 25 Apr 2016, In : Journal of Chemical Information and Modeling. 56, 4, p. 671-686 16 p.

Research output: Contribution to journalArticleResearchpeer-review

5 Citations (Scopus)

Prognostic and mechanistic potential of progesterone sulfates in intrahepatic cholestasis of pregnancy and pruritus gravidarum

Abu-Hayyeh, S., Ovadia, C., Lieu, T., Jensen, D. D., Chambers, J., Dixon, P. H., Lovgren-Sandblom, A., Bolier, R., Tolenaars, D., Kremer, A. E., Syngelaki, A., Noori, M., Williams, D., Marin, J. J. G., Monte, M. J., Nicolaides, K. H., Beuers, U. H. W., Oude-Elferink, R., Seed, P. T., Chappell, L. & 3 others, Marschall, H-U., Bunnett, N. W. & Williamson, C., 2016, In : Hepatology. 63, 4, p. 1287-1298 12 p.

Research output: Contribution to journalArticleResearchpeer-review

41 Citations (Scopus)

Proposed mode of binding and action of positive allosteric modulators at opioid receptors

Shang, Y., Yeatman, H. R., Provasi, D., Alt, A., Christopoulos, A., Canals, M. & Filizola, M., 20 May 2016, In : ACS Chemical Biology. 11, 5, p. 1220-1229 10 p.

Research output: Contribution to journalArticleResearchpeer-review

30 Citations (Scopus)

Protein kinase D and Gβγ subunits mediate agonist-evoked translocation of protease-activated receptor-2 from the golgi apparatus to the plasma membrane

Jensen, D. D., Zhao, P., Jimenez-Vargas, N. N., Lieu, T., Gerges, M., Yeatman, H. R., Canals, M., Vanner, S. J., Poole, D. P. & Bunnett, N. W., 20 May 2016, In : The Journal of Biological Chemistry. 291, 21, p. 11285-11299 15 p.

Research output: Contribution to journalArticleResearchpeer-review

9 Citations (Scopus)

Quantification of adenosine A1 receptor biased agonism: Implications for drug discovery

Baltos, J-A., Gregory, K. J., White, P. J., Sexton, P. M., Christopoulos, A. & May, L. T., 1 Jan 2016, In : Biochemical Pharmacology. 99, p. 101-112 12 p.

Research output: Contribution to journalArticleResearchpeer-review

29 Citations (Scopus)

Role of the second extracellular loop of the adenosine A1 receptor on allosteric modulator binding, signaling, and cooperativity

Nguyen, A. T. N., Vecchio, E. A., Thomas, T., Nguyen, T. D., Aurelio, L., Scammells, P. J., White, P. J., Sexton, P. M., Gregory, K. J., May, L. T. & Christopoulos, A., 1 Dec 2016, In : Molecular Pharmacology. 90, 6, p. 715-725 11 p.

Research output: Contribution to journalArticleResearchpeer-review

25 Citations (Scopus)

Sarcolemmal dependence of cardiac protection and stress-resistance: roles in aged or diseased hearts

See Hoe, L. E., May, L. T., Headrick, J. P. & Peart, J. N., Oct 2016, In : British Journal of Pharmacology. 173, 20, p. 2966-2991 26 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

4 Citations (Scopus)

Sickness behavior induced by cisplatin chemotherapy and radiotherapy in a murine head and neck cancer model is associated with altered mitochondrial gene expression

Vichaya, E. G., Molkentine, J. M., Vermeer, D. W., Walker, A. K., Feng, R., Holder, G., Luu, K., Mason, R. M., Saligan, L., Heijnen, C. J., Kavelaars, A., Mason, K. A., Lee, J. H. & Dantzer, R., 15 Jan 2016, In : Behavioural Brain Research. 297, p. 241-250 10 p.

Research output: Contribution to journalArticleResearchpeer-review

12 Citations (Scopus)

Stress-driven lymphatic dissemination: An unanticipated consequence of communication between the sympathetic nervous system and lymphatic vasculature

Le, C. P. & Sloan, E. K., 3 Jul 2016, In : Molecular & Cellular Oncology. 3, 4, 3 p., e1177674.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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1 Citation (Scopus)

Structure-activity analysis of biased agonism at the human adenosine A3 receptor

Baltos, J-A., Paoletta, S., Nguyen, A. T. N., Gregory, K. J., Tosh, D. K., Christopoulos, A., Jacobson, K. A. & May, L. T., 1 Jul 2016, In : Molecular Pharmacology. 90, 1, p. 12-22 11 p.

Research output: Contribution to journalArticleResearchpeer-review

24 Citations (Scopus)

Systematic analysis of factors influencing observations of biased agonism at the mu-opioid receptor

Thompson, G. L., Lane, J. R., Coudrat, T., Sexton, P. M., Christopoulos, A. & Canals, M., 1 Aug 2016, In : Biochemical Pharmacology. 113, p. 70-87 18 p.

Research output: Contribution to journalArticleResearchpeer-review

34 Citations (Scopus)

The A2b adenosine receptor antagonist PSB-603 promotes oxidative phosphorylation and ROS production in colorectal cancer cells via adenosine receptor-independent mechanism

Mølck, C., Ryall, J., Failla, L. M., Coates, J. L., Pascussi, J. M., Heath, J. K., Stewart, G. & Hollande, F., 1 Dec 2016, In : Cancer Letters. 383, 1, p. 135-143 9 p.

Research output: Contribution to journalArticleResearchpeer-review

13 Citations (Scopus)
Open Access
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18 Citations (Scopus)

The complexity of signalling mediated by the glucagon-like peptide-1 receptor

Fletcher, M. M., Halls, M. L., Christopoulos, A., Sexton, P. M. & Wootten, D., 15 Apr 2016, In : Biochemical Society Transactions. 44, 2, p. 582-588 7 p.

Research output: Contribution to journalArticleResearchpeer-review

8 Citations (Scopus)

The C-terminus of the B-chain of human insulin-like peptide 5 is critical for cognate RXFP4 receptor activity

Patil, N. A., Bathgate, R. A. D., Kocan, M., Ang, S. Y., Tailhades, J., Separovic, F., Summers, R., Grosse, J., Hughes, R. A., Wade, J. D. & Hossain, M. A., 1 Apr 2016, In : Amino Acids. 48, 4, p. 987-992 6 p.

Research output: Contribution to journalArticleResearchpeer-review

8 Citations (Scopus)

The extracellular surface of the GLP-1 receptor is a molecular trigger for biased agonism

Wootten, D., Reynolds, C. A., Smith, K. J., Mobarec, J. C., Koole, C., Savage, E. E., Pabreja, K., Simms, J., Sridhar, R., Furness, S. G. B., Liu, M., Thompson, P. E., Miller, L. J., Christopoulos, A. & Sexton, P. M., 16 Jun 2016, In : Cell. 165, 7, p. 1632-1643 12 p.

Research output: Contribution to journalArticleResearchpeer-review

65 Citations (Scopus)

The Helix-Loop-Helix Protein ID2 Governs NK Cell Fate by Tuning Their Sensitivity to Interleukin-15

Delconte, R. B., Shi, W., Sathe, P., Ushiki, T., Seillet, C., Minnich, M., Kolesnik, T. B., Rankin, L. C., Mielke, L. A., Zhang, J-G., Busslinger, M., Smyth, M. J., Hutchinson, D. S., Nutt, S. L., Nicholson, S. E., Alexander, W. S., Corcoran, L. M., Vivier, E., Belz, G. T., Carotta, S. & 1 others, Huntington, N. D., 19 Jan 2016, In : Immunity. 44, 1, p. 103-115 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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57 Citations (Scopus)

The hybrid molecule, VCP746, is a potent adenosine A2B receptor agonist that stimulates anti-fibrotic signalling

Vecchio, L., Chuo, C. H., Baltos, J-A., Ford, L., Scammells, P. J., Wang, B. H., Christopoulos, A., White, P. J. & May, L. T., 1 Oct 2016, In : Biochemical Pharmacology. 117, p. 46-56 11 p.

Research output: Contribution to journalArticleResearchpeer-review

15 Citations (Scopus)

The role of kinetic context in apparent biased agonism at GPCRs

Herenbrink, C. K., Sykes, D. A., Donthamsetti, P., Canals, M., Coudrat, T., Shonberg, J., Scammells, P. J., Capuano, B., Sexton, P. M., Charlton, S. J., Javitch, J. A., Christopoulos, A. & Lane, J. R., 24 Feb 2016, In : Nature Communications. 7, 14 p., 10842.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
147 Citations (Scopus)

The β2-adrenoceptor activates a positive cAMP-calcium feedforward loop to drive breast cancer cell invasion

Pon, C., Lane, J. R. D., Sloan, E. K. & Halls, M., 2016, In : The FASEB Journal. 30, 3, p. 1144-1154 11 p.

Research output: Contribution to journalArticleResearchpeer-review

25 Citations (Scopus)

Tissue-specific calibration of real-time PCR facilitates absolute quantification of plasmid DNA in biodistribution studies

Ho, J. K., White, P. J. & Pouton, C. W., 4 Oct 2016, In : Molecular Therapy - Nucleic Acids. 5, 10, 9 p., e371.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
1 Citation (Scopus)

Toward community standards and software for whole-cell modeling

Waltemath, D., Karr, J. R., Bergmann, F. T., Chelliah, V., Hucka, M., Krantz, M., Liebermeister, W., Mendes, P., Myers, C. J., Pir, P., Alaybeyoglu, B., Aranganathan, N. K., Baghalian, K., Bittig, A. T., Burke, P. E. P., Cantarelli, M., Chew, Y. H., Costa, R. S., Cursons, J., Czauderna, T. & 37 others, Goldberg, A. P., Gomez, H. F., Hahn, J., Hameri, T., Gardiol, D. F. H., Kazakiewicz, D., Kiselev, I., Knight-Schrijver, V., Knupfer, C., Konig, M., Lee, D., Lloret-Villas, A., Mandrik, N., Medley, J. K., Moreau, B., Naderi-Meshkin, H., Palaniappan, S. K., Priego-Espinosa, D., Scharm, M., Sharma, M., Smallbone, K., Stanford, N. J., Song, J-H., Theile, T., Tokic, M., Tomar, N., Toure, V., Uhlendorf, J., Varusai, T. M., Watanabe, L. H., Wendland, F., Wolfien, M., Yurkovich, J. T., Zhu, Y., Zardilis, A., Zhukova, A. & Schreiber, F., 1 Oct 2016, In : IEEE Transactions on Biomedical Engineering. 63, 10, p. 2007-2014 8 p., 7489010.

Research output: Contribution to journalArticleResearchpeer-review

27 Citations (Scopus)

Towards a structural understanding of allosteric drugs at the human calcium-sensing receptor

Leach, K., Gregory, K., Kufareva, I., Khajehali, E., Cook, A. E., Abagyan, R., Conigrave, A. D., Sexton, P. M. & Christopoulos, A., 1 May 2016, In : Cell Research. 26, 5, p. 574-592 19 p.

Research output: Contribution to journalArticleResearchpeer-review

41 Citations (Scopus)

Use of cysteine trapping to map spatial approximations between residues contributing to the helix N-capping motif of secretin and distinct residues within each of the extracellular loops of its receptor

Dong, M., Lam, P. C. H., Orry, A., Sexton, P. M., Christopoulos, A., Abagyan, R. & Miller, L. J., 4 Mar 2016, In : The Journal of Biological Chemistry. 291, 10, p. 5172-5184 13 p.

Research output: Contribution to journalArticleResearchpeer-review

7 Citations (Scopus)
13 Citations (Scopus)

β2-adrenoceptors on tumor cells play a critical role in stress-enhanced metastasis in a mouse model of breast cancer

Chang, A., Le, C. P., Walker, A. K., Creed, S. J., Pon, C. K., Albold, S., Carroll, D., Halls, M. L., Lane, J. R., Riedel, B., Ferrari, D. & Sloan, E. K., 1 Oct 2016, In : Brain, Behavior, and Immunity. 57, p. 106-115 10 p.

Research output: Contribution to journalArticleResearchpeer-review

28 Citations (Scopus)

β-adrenergic-stimulated macrophages: comprehensive localization in the M1-M2 spectrum

Lamkin, D. M., Ho, H-Y., Ong, T. H., Kawanishi, C. K., Stoffers, V. L., Ahlawat, N., Ma, J. C. Y., Arevalo, J. M. G., Cole, S. W. & Sloan, E. K., 1 Oct 2016, In : Brain, Behavior, and Immunity. 57, p. 338-346 9 p.

Research output: Contribution to journalArticleResearchpeer-review

25 Citations (Scopus)

β-arrestin-biased agonists of the GLP-1 receptor from β-amino acid residue incorporation into GLP-1 analogues

Hager, M. V., Johnson, L. M., Wootten, D., Sexton, P. M. & Gellman, S. H., 16 Nov 2016, In : Journal of the American Chemical Society. 138, 45, p. 14970-14979 10 p.

Research output: Contribution to journalArticleResearchpeer-review

35 Citations (Scopus)