Research Output

2019

Exploring use of unsupervised clustering to associate signaling profiles of GPCR ligands to clinical response

Benredjem, B., Gallion, J., Pelletier, D., Dallaire, P., Charbonneau, J., Cawkill, D., Nagi, K., Gosink, M., Lukasheva, V., Jenkinson, S., Ren, Y., Somps, C., Murat, B., Van Der Westhuizen, E., Le Gouill, C., Lichtarge, O., Schmidt, A., Bouvier, M. & Pineyro, G., 9 Sep 2019, In : Nature Communications. 10, 1, 15 p., 4075.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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2 Citations (Scopus)

Expression and activity of the calcitonin receptor family in a sample of primary human high-grade gliomas

Ostrovskaya, A., Hick, C., Hutchinson, D. S., Stringer, B. W., Wookey, P. J., Wootten, D., Sexton, P. M. & Furness, S. G. B., 18 Feb 2019, In : BMC Cancer. 19, 1, 12 p., 157.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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1 Citation (Scopus)

G-Protein–Coupled Receptors Are Dynamic Regulators of Digestion and Targets for Digestive Diseases

Canals, M., Poole, D. P., Veldhuis, N. A., Schmidt, B. L. & Bunnett, N. W., 1 May 2019, In : Gastroenterology. 156, 6, p. 1600-1616 17 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

3 Citations (Scopus)
Open Access
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1 Citation (Scopus)

GRK mediates µ-opioid receptor plasma membrane reorganization

Gondin, A. B., Halls, M. L., Canals, M. & Briddon, S. J., 1 May 2019, In : Frontiers in Molecular Neuroscience. 12, 14 p., 104.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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4 Citations (Scopus)

How an activation signal is transmitted through an excitatory receptor

Gregory, K. J., 7 Feb 2019, In : Nature. 566, 7742, p. 42-43 2 p.

Research output: Contribution to journalArticleOtherpeer-review

I8-arachnotocin–an arthropod-derived G protein-biased ligand of the human vasopressin V2 receptor

Duerrauer, L., Muratspahić, E., Gattringer, J., Keov, P., Mendel, H. C., Pfleger, K. D. G., Muttenthaler, M. & Gruber, C. W., 17 Dec 2019, In : Scientific Reports. 9, 1, 11 p., 19295.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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2 Citations (Scopus)

Interaction of neurotransmitters and neurochemicals with lymphocytes

Kerage, D., Sloan, E. K., Mattarollo, S. R. & McCombe, P. A., 15 Jul 2019, In : Journal of Neuroimmunology. 332, p. 99-111 13 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

Open Access
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5 Citations (Scopus)

Internalized GPCRs as Potential Therapeutic Targets for the Management of Pain

Retamal, J. S., Ramírez-García, P. D., Shenoy, P. A., Poole, D. P. & Veldhuis, N. A., 12 Nov 2019, In : Frontiers in Molecular Neuroscience. 12, p. 1-10 10 p., 273.

Research output: Contribution to journalReview ArticleResearchpeer-review

Open Access
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1 Citation (Scopus)

Intra-articular Treatment of Osteoarthritis with Diclofenac-Conjugated Polymer Reduces Inflammation and Pain

Sulistio, A., Mansfeld, F. M., Reyes-Ortega, F., D'Souza, A. M., Ng, S. M. Y., Birkett, S., Blencowe, A., Qiao, G. G., Little, C. B., Shu, C. C., Bendele, A. M., Valade, D., Donohue, A. C., Quinn, J. F., Whittaker, M. R., Davis, T. P. & Tait, R. J., 24 May 2019, In : ACS Applied Bio Materials. 2, 7, p. 2822-2832 11 p.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

IRAK3 modulates downstream innate immune signalling through its guanylate cyclase activity

Freihat, L. A., Wheeler, J. I., Wong, A., Turek, I., Manallack, D. T. & Irving, H. R., Oct 2019, In : Scientific Reports. 9, 12 p., 15468.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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1 Citation (Scopus)

Isolation, Purification, Generation, and Culture of Osteocytes

Gooi, J. H., Chia, L. Y., Vrahnas, C. & Sims, N. A., 1 Jan 2019, Bone Research Protocols. Idris, A. I. (ed.). 3 ed. New York NY USA: Humana Press, Vol. 1914. p. 39-51 13 p. (Methods in Molecular Biology; vol. 1914, no. 3).

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

1 Citation (Scopus)

Kinetic and system bias as drivers of metabotropic glutamate receptor 5 allosteric modulator pharmacology

Sengmany, K., Hellyer, S. D., Albold, S., Wang, T., Conn, P. J., May, L. T., Christopoulos, A., Leach, K. & Gregory, K. J., 1 May 2019, In : Neuropharmacology. 149, p. 83-96 14 p.

Research output: Contribution to journalArticleResearchpeer-review

8 Citations (Scopus)

L-Amino Acids Promote Calcitonin Release via a Calcium-Sensing Receptor: Gq/11-Mediated Pathway in Human C-Cells

Mun, H. C., Leach, K. M. & Conigrave, A. D., 1 Jan 2019, In : Endocrinology. 160, 7, p. 1590-1599 10 p.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

Ligand-dependent spatiotemporal signaling profiles of the μ-opioid receptor are controlled by distinct protein-interaction networks

Civciristov, S., Huang, C., Liu, B., Marquez, E. A., Gondin, A. B., Schittenhelm, R. B., Ellisdon, A. M., Canals, M. & Halls, M. L., 1 Nov 2019, In : The Journal of Biological Chemistry. 294, 44, p. 16198-16213 16 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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1 Citation (Scopus)

Light-activated chimeric GPCRs: limitations and opportunities

Tichy, A-M., Gerrard, E. J., Sexton, P. M. & Janovjak, H., 1 Aug 2019, In : Current Opinion in Structural Biology. 57, p. 196-203 8 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

2 Citations (Scopus)

Localised GPCR signalling as revealed by FRET biosensors

Halls, M. L., 1 Apr 2019, In : Current Opinion in Cell Biology. 57, p. 48-56 9 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

7 Citations (Scopus)

Loss of O-Linked Protein Glycosylation in Burkholderia cenocepacia Impairs Biofilm Formation and Siderophore Activity and Alters Transcriptional Regulators

Oppy, C. C., Jebeli, L., Kuba, M., Oates, C. V., Strugnell, R., Edgington-Mitchell, L. E., Valvano, M. A., Hartland, E. L., Newton, H. J. & Scott, N. E., 13 Nov 2019, In : mSphere. 4, 6, 22 p., e00660-19.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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Metabolic control and sex: A focus on inflammatory-linked mediators

Henstridge, D. C., Abildgaard, J., Lindegaard, B. & Febbraio, M. A., 28 Feb 2019, In : British Journal of Pharmacology. 176, 21, p. 4193-4207 15 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

7 Citations (Scopus)

Metabotropic glutamate receptor 5 (mGlu5)-positive allosteric modulators differentially induce or potentiate desensitization of mGlu5 signaling in recombinant cells and neurons

Hellyer, S. D., Albold, S., Sengmany, K., Singh, J., Leach, K. & Gregory, K. J., 1 Jan 2019, In : Journal of Neurochemistry. 151, 3, p. 301-315 15 p.

Research output: Contribution to journalArticleResearchpeer-review

3 Citations (Scopus)

Microfluidic preparation of drug-loaded PEGylated liposomes, and the impact of liposome size on tumour retention and penetration

Dong, Y. D., Tchung, E., Nowell, C., Kaga, S., Leong, N., Mehta, D., Kaminskas, L. M. & Boyd, B. J., 2019, In : Journal of Liposome Research. 29, 1, p. 1-9 9 p.

Research output: Contribution to journalArticleResearchpeer-review

13 Citations (Scopus)

Molecular Basis of Action of a Small-Molecule Positive Allosteric Modulator Agonist at the Type 1 Cholecystokinin Holoreceptor

Desai, A. J., Mechin, I., Nagarajan, K., Valant, C., Wootten, D., Lam, P. C. H., Orry, A., Abagyan, R., Nair, A., Sexton, P. M., Christopoulos, A. & Miller, L. J., 1 Mar 2019, In : Molecular Pharmacology. 95, 3, p. 245-259 15 p.

Research output: Contribution to journalArticleResearchpeer-review

Molecular Determinants of the Intrinsic Efficacy of the Antipsychotic Aripiprazole

Klein Herenbrink, C., Verma, R., Lim, H. D., Kopinathan, A., Keen, A., Shonberg, J., Draper-Joyce, C. J., Scammells, P. J., Christopoulos, A., Javitch, J. A., Capuano, B., Shi, L. & Lane, J. R., 16 Aug 2019, In : ACS Chemical Biology. 14, 8, p. 1780-1792 13 p.

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)

O-GlcNAc Engineering of GPCR Peptide-Agonists Improves Their Stability and in Vivo Activity

Levine, P. M., Balana, A. T., Sturchler, E., Koole, C., Noda, H., Zarzycka, B., Daley, E. J., Truong, T., Katritch, V., Gardella, T. J., Wootten, D., Sexton, P. M., McDonald, P. & Pratt, M. R., 11 Sep 2019, In : Journal of the American Chemical Society. 141, 36, p. 14210-14219 10 p.

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)

Overcoming P-Glycoprotein-Mediated Drug Resistance with Noscapine Derivatives

Muthiah, D., Henshaw, G. K., DeBono, A. J., Capuano, B., Scammells, P. J. & Callaghan, R., 1 Feb 2019, In : Drug Metabolism and Disposition. 47, 2, p. 164-172 9 p.

Research output: Contribution to journalArticleResearchpeer-review

6 Citations (Scopus)

Preclinical Models for Studying NASH-Driven HCC: How Useful Are They?

Febbraio, M. A., Reibe, S., Shalapour, S., Ooi, G. J., Watt, M. J. & Karin, M., 8 Jan 2019, In : Cell Metabolism. 29, 1, p. 18-26 9 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

26 Citations (Scopus)

Protein kinase D and Gβγ mediate sustained nociceptive signaling by biased agonists of protease-activated receptor-2

Zhao, P., Pattison, L. A., Jensen, D. D., Jimenez-Vargas, N. N., Latorre, R., Lieu, T., Jaramillo, J. O., Lopez-Lopez, C., Poole, D. P., Vanner, S. J., Schmidt, B. L. & Bunnett, N. W., 5 Jul 2019, In : The Journal of Biological Chemistry. 294, 27, p. 10649-10662 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Rapid Assessment of Nanoparticle Extravasation in a Microfluidic Tumor Model

Vu, N. M., Rajasekhar, P., Poole, D. P., Khor, S. Y., Truong Phuoc, N., Nowell, C., Quinn, J. F., Whittaker, M., Veldhuis, N. & Davis, T. P., 29 Mar 2019, In : ACS Applied Nano Materials. 2, 4, p. 1844-1856 13 p.

Research output: Contribution to journalArticleResearchpeer-review

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4 Citations (Scopus)

Relieving ER stress to target NASH-driven hepatocellular carcinoma

Reibe, S. & Febbraio, M. A., 1 Feb 2019, In : Nature Reviews Endocrinology. 15, 2, p. 73-74 2 p.

Research output: Contribution to journalReview ArticleOtherpeer-review

Open Access
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2 Citations (Scopus)

Research Tool Helps Validate Efficacy of Functional Foods

Buecking, M., Goeckener, B., Haynes, J., Leitner, P., Murray, M., Williamson, G. & Bennett, L. E., 1 Nov 2019, Food Technology 18 p.

Research output: Contribution to specialist publicationArticleOther

Signalling in response to sub-picomolar concentrations of active compounds: Pushing the boundaries of GPCR sensitivity

Civciristov, S. & Halls, M. L., Jul 2019, In : British Journal of Pharmacology. 176, 14, p. 2382-2401 20 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

2 Citations (Scopus)

Social behaviour is altered in the insulin-regulated aminopeptidase knockout mouse

Burns, P., Bowditch, J., McFadyen, J., Loiacono, R., Albiston, A. L., Pham, V. & Chai, S. Y., 30 Dec 2019, In : Behavioural Brain Research. 376, 7 p., 112150.

Research output: Contribution to journalArticleResearchpeer-review

Stress hormone signaling through β-adrenergic receptors regulates macrophage mechanotype and function

Kim, T. H., Ly, C., Christodoulides, A., Nowell, C. J., Gunning, P. W., Sloan, E. K. & Rowat, A. C., Mar 2019, In : The FASEB Journal. 33, 3, p. 3997-4006 10 p.

Research output: Contribution to journalArticleResearchpeer-review

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5 Citations (Scopus)

Structure-Kinetic Profiling of Haloperidol Analogues at the Human Dopamine D2 Receptor

Fyfe, T., Kellam, B., Sykes, D. A., Capuano, B., Scammells, P., Lane, R., Charlton, S. J. & Mistry, S., 14 Nov 2019, In : Journal of Medicinal Chemistry. 62, 21, p. 9488-9520 33 p.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

Structure of Pseudomonas aeruginosa ribosomes from an aminoglycoside-resistant clinical isolate

Halfon, Y., Jimenez-Fernandez, A., Rosa, R. L., Portero, R. E., Johansen, H. K., Matzov, D., Eyal, Z., Bashan, A., Zimmerman, E., Belousoff, M., Molin, S. & Yonath, A., 29 Oct 2019, In : Proceedings of the National Academy of Sciences of the United States of America. 116, 44, p. 22275-22281 7 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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4 Citations (Scopus)

Substituted Pyridazin-3(2 H)-ones as Highly Potent and Biased Formyl Peptide Receptor Agonists

Deora, G. S., Qin, C. X., Vecchio, E. A., Debono, A. J., Priebbenow, D. L., Brady, R. M., Beveridge, J., Teguh, S. C., Deo, M., May, L. T., Krippner, G., Ritchie, R. H. & Baell, J. B., 23 May 2019, In : Journal of Medicinal Chemistry. 62, 10, p. 5242-5248 7 p.

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)

Subtle modifications to a thieno[2,3-d]pyrimidine scaffold yield negative allosteric modulators and agonists of the dopamine D 2 receptor

Fyfe, T. J., Kellam, B., Mistry, S. N., Scammells, P. J., Lane, J. R. & Capuano, B., 15 Apr 2019, In : European Journal of Medicinal Chemistry. 168, p. 474-490 17 p.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

Tetrahydroquinoxalines induce a lethal evisceration phenotype in Haemonchus contortus in vitro

Jiao, Y., Preston, S., Garcia-Bustos, J. F., Baell, J. B., Ventura, S., Le, T., McNamara, N., Nguyen, N., Botteon, A., Skinner, C., Danne, J., Ellis, S., Koehler, A. V., Wang, T., Chang, B. C. H., Hofmann, A., Jabbar, A. & Gasser, R. B., 1 Apr 2019, In : International Journal for Parasitology: Drugs and Drug Resistance. 9, p. 59-71 13 p.

Research output: Contribution to journalArticleResearchpeer-review

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6 Citations (Scopus)

The adenosine A 2B G protein-coupled receptor: Recent advances and therapeutic implications

Vecchio, E. A., White, P. J. & May, L. T., 1 Jan 2019, In : Pharmacology and Therapeutics. 198, p. 20-33 14 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

7 Citations (Scopus)

The concise guide to Pharmacology 2019/20: G protein-coupled receptors

Alexander, S. P. H., Christopoulos, A., Davenport, A. P., Kelly, E., Mathie, A., Peters, J. A., Veale, E. L., Armstrong, J. F., Faccenda, E., Harding, S. D., Pawson, A. J., Sharman, J. L., Southan, C., Davies, J. A. & CGTP Collaborators, 1 Dec 2019, In : British Journal of Pharmacology. 176, S1, p. S21-S141 120 p.

Research output: Contribution to journalArticleOtherpeer-review

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147 Citations (Scopus)

The Effects of Clioquinol on P-glycoprotein Expression and Biometal Distribution in the Mouse Brain Microvasculature

McInerney, M. P., Pan, Y., Volitakis, I., Bush, A. I., Short, J. L. & Nicolazzo, J. A., Dec 2019, In : Journal of Pharmaceutical Sciences. 108, 7, p. 2247-2255 9 p.

Research output: Contribution to journalArticleResearchpeer-review

3 Citations (Scopus)

The importance of sex differences in pharmacology research

Gogos, A., Langmead, C., Sullivan, J. C. & Lawrence, A. J., 1 Nov 2019, In : British Journal of Pharmacology. 176, 21, p. 4087-4089 3 p.

Research output: Contribution to journalEditorialOther

Open Access
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1 Citation (Scopus)

The Molecular Control of Calcitonin Receptor Signaling

dal Maso, E., Glukhova, A., Zhu, Y., Garcia-Nafria, J., Tate, C. G., Atanasio, S., Reynolds, C. A., Ramirez-Aportela, E., Carazo, J-M., Hick, C. A., Furness, S. G. B., Hay, D. L., Liang, Y-L., Miller, L. J., Christopoulos, A., Wang, M-W., Wootten, D. & Sexton, P. M., 8 Feb 2019, In : ACS Pharmacology & Translational Science. 2, 1, p. 31-51 21 p.

Research output: Contribution to journalArticleResearchpeer-review

16 Citations (Scopus)

The nature of efficacy at G protein-coupled receptors

Zhao, P. & Furness, S. G. B., 1 Dec 2019, In : Biochemical Pharmacology. 170, 113647.

Research output: Contribution to journalReview ArticleResearchpeer-review

2 Citations (Scopus)

Therapeutic blockade of activin-A improves NK cell function and antitumor immunity

Rautela, J., Dagley, L. F., De Oliveira, C. C., Schuster, I. S., Hediyeh-Zadeh, S., Delconte, R. B., Cursons, J., Hennessy, R., Hutchinson, D. S., Harrison, C., Kita, B., Vivier, E., Webb, A. I., Degli-Esposti, M. A., Davis, M. J., Huntington, N. D. & Souza-Fonseca-Guimaraes, F., 27 Aug 2019, In : Science Signaling. 12, 596, 13 p., aat7527.

Research output: Contribution to journalArticleResearchpeer-review

9 Citations (Scopus)

Treatment of type 2 diabetes with the designer cytokine IC7Fc

Findeisen, M., Allen, T. L., Henstridge, D. C., Kammoun, H., Brandon, A. E., Baggio, L. L., Watt, K. I., Pal, M., Cron, L., Estevez, E., Yang, C., Kowalski, G. M., O’Reilly, L., Egan, C., Sun, E., Thai, L. M., Krippner, G., Adams, T. E., Lee, R. S., Grötzinger, J. & 18 others, Garbers, C., Risis, S., Kraakman, M. J., Mellet, N. A., Sligar, J., Kimber, E. T., Young, R. L., Cowley, M. A., Bruce, C. R., Meikle, P. J., Baldock, P. A., Gregorevic, P., Biden, T. J., Cooney, G. J., Keating, D. J., Drucker, D. J., Rose-John, S. & Febbraio, M. A., 25 Sep 2019, In : Nature. 574, 7776, p. 63-68 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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11 Citations (Scopus)

TrkB Agonist LM22A-4 Increases Oligodendroglial Populations During Myelin Repair in the Corpus Callosum

Nguyen, H. T. H., Wood, R. J., Prawdiuk, A. R., Furness, S. G. B., Xiao, J., Murray, S. S. & Fletcher, J. L., 27 Aug 2019, In : Frontiers in Molecular Neuroscience. 12, 12 p., 205.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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4 Citations (Scopus)

Use of Backbone Modification to Enlarge the Spatiotemporal Diversity of Parathyroid Hormone Receptor-1 Signaling via Biased Agonism

Liu, S., Jean-Alphonse, F. G., White, A. D., Wootten, D., Sexton, P. M., Gardella, T. J., Vilardaga, J. P. & Gellman, S. H., 18 Sep 2019, In : Journal of the American Chemical Society. 141, 37, p. 14486-14490 5 p.

Research output: Contribution to journalArticleResearchpeer-review

3 Citations (Scopus)