Research Output 1988 2019

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2019

6-Phenylpyrimidin-4-ones as Positive Allosteric Modulators at the M1 mAChR: The Determinants of Allosteric Activity

Jorg, M. T., van der Westhuizen, E. T., Khajehali, E., Burger, W. A. C., White, J., Choy, K. H. C., Tobin, A. B., Sexton, P. M., Valant, C., Capuano, B., Christopoulos, A. & Scammells, P. J., 20 Mar 2019, In : ACS Chemical Neuroscience. 10, 3, p. 1099-1114 16 p.

Research output: Contribution to journalArticleResearchpeer-review

A ligand-induced structural change in fatty acid-binding protein 1 is associated with potentiation of peroxisome proliferator-activated receptor α agonists

Patil, R., Mohanty, B., Liu, B., Chandrashekaran, I. R., Headey, S. J., Williams, M. L., Clements, C. S., Ilyichova, O., Doak, B. C., Genissel, P., Weaver, R., Vuillard, L., Halls, M. L., Porter, C. J. H. & Scanlon, M. J., 8 Mar 2019, In : Journal of Biological Chemistry. 294, 10, p. 3720-3734 15 p.

Research output: Contribution to journalArticleResearchpeer-review

A Nonionic Polyethylene Oxide (PEO) Surfactant Model: Experimental and Molecular Dynamics Studies of Kolliphor EL

Suys, E. J. A., Warren, D. B., Pham, A. C., Nowell, C. J., Clulow, A. J., Benameur, H., Porter, C. J. H., Pouton, C. W. & Chalmers, D. K., 1 Jan 2019, In : Journal of Pharmaceutical Sciences. 108, 1, p. 193-204 12 p.

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Circulating epinephrine is not required for chronic stress to enhance metastasis

Walker, A. K., Martelli, D., Ziegler, A. I., Lambert, G. W., Phillips, S. E., Hill, S. J., McAllen, R. M. & Sloan, E. K., 1 Jan 2019, In : Psychoneuroendocrinology. 99, p. 191-195 5 p.

Research output: Contribution to journalArticleResearchpeer-review

Identification of monellin as the first naturally-derived proteinaceous allosteric agonist of metabotropic glutamate receptor 5

Chen, A. N. Y., Hellyer, S. D., Trinh, P. N. H., Leach, K. & Gregory, K. J., 14 Apr 2019, (Accepted/In press) In : Basic and Clinical Pharmacology and Toxicology. 22 p.

Research output: Contribution to journalArticleResearchpeer-review

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

The TRPV4 Agonist GSK1016790A Regulates the Membrane Expression of TRPV4 Channels

Baratchi, S., Keov, P., Darby, W., Lai, A., Khoshmanesh, K., Thurgood, P., Vahidi, P., Ejendal, K. & McIntyre, P., 23 Jan 2019, In : Frontiers in Pharmacology. 10, 12 p., 6.

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2018

8-Mercaptoguanine Derivatives as Inhibitors of Dihydropteroate Synthase

Dennis, M. L., Lee, M. D., Harjani, J. R., Ahmed, M., Debono, A. J., Pitcher, N. P., Wang, Z-C., Chhabra, S., Barlow, N., Rahmani, R., Cleary, B., Dolezal, O., Hattarki, M., Aurelio, L., Shonberg, J., Graham, B., Peat, T. S., Baell, J. B. & Swarbrick, J. D., 6 Feb 2018, In : Chemistry - A European Journal. 24, 8, p. 1922-1930 9 p.

Research output: Contribution to journalArticleResearchpeer-review

Acute or Delayed Systemic Administration of Human Amnion Epithelial Cells Improves Outcomes in Experimental Stroke

Evans, M. A., Lim, R., Kim, H. A., Chu, H. X., Gardiner-Mann, C. V., Taylor, K. W. E., Chan, C. T., Brait, V. H., Lee, S., Dinh, Q. N., Vinh, A., Phan, T. G., Srikanth, V. K., Ma, H., Arumugam, T. V., Fann, D. Y., Poh, L., Hunt, C. P. J., Pouton, C. W., Haynes, J. M. & 12 othersSelemidis, S., Kwan, W., Teo, L., Bourne, J. A., Neumann, S., Young, S., Gowing, E. K., Drummond, G. R., Clarkson, A. N., Wallace, E. M., Sobey, C. G. & Broughton, B. R. S., 1 Mar 2018, In : Stroke. 49, 3, p. 700-709 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Allosteric interactions between GABAB1 subunits control orthosteric binding sites occupancy within GABAB oligomers

Stewart, G. D., Comps-Agrar, L., Nørskov-Lauritsen, L. B., Pin, J. P. & Kniazeff, J., 1 Jul 2018, In : Neuropharmacology. 136, p. 92-101 10 p.

Research output: Contribution to journalArticleResearchpeer-review

A Qualitative Study on the Perception of Australian and Malaysian Academic Teaching Staff in an Undergraduate B.Pharm Program on Case-based Learning

Jacob, S. A., Hui Dhing, O. & Malone, D., 2018, (Accepted/In press) In : American Journal of Pharmaceutical Education. 24 p.

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Open Access

A Structure-Activity Relationship Study of Bitopic N 6-Substituted Adenosine Derivatives as Biased Adenosine A1 Receptor Agonists

Aurelio, L., Baltos, J. A., Ford, L., Nguyen, A. T. N., Jörg, M., Devine, S. M., Valant, C., White, P. J., Christopoulos, A., May, L. T. & Scammells, P. J., 8 Mar 2018, In : Journal of Medicinal Chemistry. 61, 5, p. 2087-2103 17 p.

Research output: Contribution to journalArticleResearchpeer-review

A Thieno[2,3-d]pyrimidine Scaffold is a Novel Negative Allosteric Modulator of the Dopamine D2 Receptor

Fyfe, T. J., Zarzycka, B., Lim, H. D., Kellam, B., Mistry, S. N., Katrich, V., Scammells, P. J., Lane, J. R. & Capuano, B., 2018, (Accepted/In press) In : Journal of Medicinal Chemistry. 82 p.

Research output: Contribution to journalArticleResearchpeer-review

Characterization of signalling and regulation of common calcitonin receptor splice variants and polymorphisms

Dal Maso, E., Just, R., Hick, C., Christopoulos, A., Sexton, P. M., Wootten, D. & Furness, S. G. B., 1 Feb 2018, In : Biochemical Pharmacology. 148, p. 111-129 19 p.

Research output: Contribution to journalArticleResearchpeer-review

Cognitive benefits of lithium chloride in APP/PS1 mice are associated with enhanced brain clearance of β-amyloid

Pan, Y., Short, J. L., Newman, S. A., Choy, K. H. C., Tiwari, D., Yap, C., Senyschyn, D., Banks, W. A. & Nicolazzo, J. A., 2018, (Accepted/In press) In : Brain, Behavior, and Immunity. 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Comparative genotypic and phenotypic analysis of human peripheral blood monocytes and surrogate monocyte-like cell lines commonly used in metabolic disease research

Riddy, D. M., Goy, E., Delerive, P., Summers, R. J. & Langmead, C. J., 1 May 2018, In : PLoS ONE. 13, 5, 19 p., e0197177.

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DCC mutation update: Congenital mirror movements, isolated agenesis of the corpus callosum, and developmental split brain syndrome

Marsh, A. P. L., Edwards, T. J., Galea, C., Cooper, H. M., Engle, E. C., Jamuar, S. S., Méneret, A., Moutard, M-L., Nava, C., Rastetter, A., Robinson, G., Rouleau, G., Roze, E., Spencer-Smith, M., Trouillard, O., Billette de Villemeur, T., Walsh, C. A., Yu, T. W., IRC5 Consortium, Heron, D. & 5 othersSherr, E. H., Richards, L. J., Depienne, C., Leventer, R. J. & Lockhart, P. J., 1 Jan 2018, In : Human Mutation. 39, 1, p. 23-39 17 p.

Research output: Contribution to journalArticleResearchpeer-review

Distribution of therapeutic proteins into thoracic lymph after intravenous administration is protein size-dependent and primarily occurs within the liver and mesentery

Yadav, P., McLeod, V. M., Nowell, C. J., Selby, L. I., Johnston, A. P. R., Kaminskas, L. M. & Trevaskis, N. L., 28 Feb 2018, In : Journal of Controlled Release. 272, p. 17-28 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Evaluation and extension of the two-site, two-step model for binding and activation of the chemokine receptor CCR1

Sanchez, J., Huma, Z. E., Lane, J. R., Liu, X., Bridgford, J. L., Payne, R. J., Canals, M. & Stone, M. J., 19 Dec 2018, (Accepted/In press) In : Journal of Biological Chemistry.

Research output: Contribution to journalArticleResearchpeer-review

Extracellular loops 2 and 3 of the calcitonin receptor selectively modify agonist binding and efficacy

Dal Maso, E., Zhu, Y., Pham, V., Reynolds, C. A., Deganutti, G., Hick, C. A., Yang, D., Christopoulos, A., Hay, D. L., Wang, M. W., Sexton, P. M., Furness, S. G. B. & Wootten, D., 1 Apr 2018, In : Biochemical Pharmacology. 150, p. 214-244 31 p.

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Fluorescently Labeled Morphine Derivatives for Bioimaging Studies

Lam, R., Gondin, A. B., Canals, M., Kellam, B., Briddon, S. J., Graham, B. & Scammells, P. J., 8 Feb 2018, In : Journal of Medicinal Chemistry. 61, 3, p. 1316-1329 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Glucagon-like peptide-1 receptor internalisation controls spatiotemporal signalling mediated by biased agonists

Fletcher, M. M., Halls, M. L., Zhao, P., Clydesdale, L., Christopoulos, A., Sexton, P. M. & Wootten, D., 1 Oct 2018, In : Biochemical Pharmacology. 156, p. 406-419 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Identification of global and ligand-specific calcium sensing receptor activation mechanisms S

Keller, A., Kufareva, I., Josephs, T. M., Diao, J., Mai, V. T-V., Conigrave, A. D., Christopoulos, A., Gregory, K. J. & Leach, K., 1 Jun 2018, In : Molecular Pharmacology. 93, 6, p. 619-630 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Identification of novel antivirals inhibiting recognition of Venezuelan equine encephalitis virus capsid protein by the Importin α/β1 heterodimer through high-throughput screening

Thomas, D. R., Lundberg, L., Pinkham, C., Shechter, S., DeBono, A., Baell, J., Wagstaff, K. M., Hick, C. A., Kehn-Hall, K. & Jans, D. A., 1 Mar 2018, In : Antiviral Research. 151, p. 8-19 12 p.

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Implicating anaesthesia and the perioperative period in cancer recurrence and metastasis

Dubowitz, J. A., Sloan, E. K. & Riedel, B. J., Apr 2018, In : Clinical and Experimental Metastasis. 35, 4, p. 347-358 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Increased cardiomyocyte alignment and intracellular calcium transients using micropatterned and drug-releasing poly(glycerol sebacate) elastomers

Zhu, C., Rodda, A. E., Truong, V. X., Shi, Y., Zhou, K., Haynes, J. M., Wang, B., Cook, W. D. & Forsythe, J. S., 2018, In : ACS Biomaterials Science and Engineering. 4, 7, p. 2494-2504 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Induced pluripotent stem cell-derived podocyte-like cells as models for assessing mechanisms underlying heritable disease phenotype: Initial studies using two alport syndrome patient lines indicate impaired potassium channel activity

Haynes, J. M., Selby, J. N., Vandekolk, T. H., Abad, I. P. L., Ho, J. K., Lieuw, W-L., Leach, K., Savige, J., Saini, S., Fisher, C. L. & Ricardo, S. D., 1 Nov 2018, In : Journal of Pharmacology and Experimental Therapeutics. 367, 2, p. 335-347 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Inflammation-associated changes in DOR expression and function in the mouse colon

Dicello, J. J., Saito, A., Rajasekhar, P., Eriksson, E. M., McQuade, R., Nowell, C., Sebastian, B., Fichna, J., Veldhuis, N. A., Canals, M., Bunnett, N., Carbone, S. E. & Poole, D. P., 1 Oct 2018, In : American Journal of Physiology - Gastrointestinal and Liver Physiology. 315, 4, p. G544-G559 39 p.

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INSL5 activates multiple signalling pathways and regulates GLP-1 secretion in NCI-H716 cells

Ang, S. Y., Evans, B. A., Poole, D. P., Bron, R., DiCello, J. J., Bathgate, R. A. D., Kocan, M., Hutchinson, D. S. & Summers, R. J., 1 Apr 2018, In : Journal of Molecular Endocrinology. 60, 3, p. 213-224 12 p.

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Ionophore and Biometal Modulation of P-glycoprotein Expression and Function in Human Brain Microvascular Endothelial Cells

McInerney, M. P., Volitakis, I., Bush, A. I., Banks, W. A., Short, J. L. & Nicolazzo, J. A., 1 Apr 2018, In : Pharmaceutical Research. 35, 4, 12 p., 83.

Research output: Contribution to journalArticleResearchpeer-review

MACROD2 haploinsufficiency impairs catalytic activity of PARP1 and promotes chromosome instability and growth of intestinal tumors

Sakthianandeswaren, A., Parsons, M. J., Mouradov, D., Mackinnon, R. N., Catimel, B., Liu, S., Palmieri, M., Love, C., Jorissen, R. N., Li, S., Whitehead, L., Putoczki, T. L., Preaudet, A., Tsui, C., Nowell, C. J., Ward, R. L., Hawkins, N. J., Desai, J., Gibbs, P., Ernst, M. & 3 othersStreet, I., Buchert, M. & Sieber, O. M., 1 Aug 2018, In : Cancer Discovery. 8, 8, p. 988-1005 18 p.

Research output: Contribution to journalArticleResearchpeer-review

Muscarinic M5 receptors modulate ethanol seeking in rats

Berizzi, A. E., Perry, C. J., Shackleford, D. M., Lindsley, C. W., Jones, C. K., Chen, N. A., Sexton, P. M., Christopoulos, A., Langmead, C. J. & Lawrence, A. J., 1 Jun 2018, In : Neuropsychopharmacology. 43, 7, p. 1510-1517 8 p.

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NKX2-5 regulates human cardiomyogenesis via a HEY2 dependent transcriptional network

Anderson, D. J., Kaplan, D. I., Bell, K. M., Koutsis, K., Haynes, J. M., Mills, R. J., Phelan, D. G., Qian, E. L., Leitoguinho, A. R., Arasaratnam, D., Labonne, T., Ng, E. S., Davis, R. P., Casini, S., Passier, R., Hudson, J. E., Porrello, E. R., Costa, M. W., Rafii, A., Curl, C. L. & 9 othersDelbridge, L. M., Harvey, R. P., Oshlack, A., Cheung, M. M., Mummery, C. L., Petrou, S., Elefanty, A. G., Stanley, E. G. & Elliott, D. A., 10 Apr 2018, In : Nature Communications. 9, 1, 13 p., 1373.

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Novel imaging of the prostate reveals spontaneous gland contraction and excretory duct quiescence together with different drug effects

Kügler, R., Mietens, A., Seidensticker, M., Tasch, S., Wagenlehner, F. M., Kaschtanow, A., Tjahjono, Y., Tomczyk, C. U., Beyer, D., Risbridger, G. P., Exintaris, B., Ellem, S. J. & Middendorff, R., 1 Mar 2018, In : FASEB Journal. 32, 3, p. 1130-1138 9 p.

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Phase-plate cryo-EM structure of a biased agonistbound human GLP-1 receptor-Gs complex

Liang, Y. L., Khoshouei, M., Glukhova, A., Furness, S. G. B., Zhao, P., Clydesdale, L., Koole, C., Truong, T. T., Thal, D. M., Lei, S., Radjainia, M., Danev, R., Baumeister, W., Wang, M. W., Miller, L. J., Christopoulos, A., Sexton, P. M. & Wootten, D., 1 Mar 2018, In : Nature. 555, 7694, p. 121-125 5 p.

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Polymyxin B causes DNA damage in HK-2 cells and mice

Yun, B., Zhang, T., Azad, M. A. K., Wang, J., Nowell, C. J., Kalitsis, P., Velkov, T., Hudson, D. F. & Li, J., Jul 2018, In : Archives of Toxicology. 92, 7, p. 2259-2271 13 p.

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Preassembled GPCR signaling complexes mediate distinct cellular responses to ultralow ligand concentrations

Civciristov, S., Ellisdon, A. M., Suderman, R., Pon, C. K., Evans, B. A., Kleifeld, O., Charlton, S. J., Hlavacek, W. S., Canals, M. & Halls, M. L., 9 Oct 2018, In : Science Signaling. 11, 551, 22 p., eaan1188.

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Predicting cancer cell invasion by single-cell physical phenotyping

Nyberg, K. D., Bruce, S. L., Nguyen, A. V., Chan, C. K., Gill, N. K., Kim, T. H., Sloan, E. K. & Rowat, A. C., 1 Apr 2018, In : Integrative Biology: Quantitative Biosciences from Nano to Macro. 10, 4, p. 218-231 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Protease-activated receptor-2 in endosomes signals persistent pain of irritable bowel syndrome

Jimenez-Vargas, N. N., Pattison, L. A., Zhao, P., Lieu, T., Latorre, R., Jensen, D. D., Castro, J., Aurelio, L., Le, G. T., Flynn, B., Herenbrink, C. K., Yeatman, H. R., Edgington-Mitchell, L., Porter, C. J. H., Halls, M. L., Canals, M., Veldhuis, N. A., Poole, D. P., McLean, P., Hicks, G. A. & 7 othersScheff, N., Chen, E., Bhattacharya, A., Schmidt, B. L., Brierley, S. M., Vanner, S. J. & Bunnett, N. W., 31 Jul 2018, In : Proceedings of the National Academy of Sciences of the United States of America. 115, 31, p. E7438-E7447 10 p.

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Proteomic Identification of Interferon-Induced Proteins with Tetratricopeptide Repeats as Markers of M1 Macrophage Polarization

Huang, C., Lewis, C., Borg, N. A., Canals, M., Diep, H., Drummond, G. R., Goode, R. J., Schittenhelm, R. B., Vinh, A., Zhu, M., Kemp-Harper, B., Kleifeld, O. & Stone, M. J., 6 Apr 2018, In : Journal of Proteome Research. 17, 4, p. 1485-1499 15 p.

Research output: Contribution to journalArticleResearchpeer-review

Rosiglitazone and a β3-adrenoceptor agonist are both required for functional browning of white adipocytes in culture

Merlin, J., Sato, M., Chia, L. Y., Fahey, R., Pakzad, M., Nowell, C. J., Summers, R. J., Bengtsson, T., Evans, B. A. & Hutchinson, D. S., 30 May 2018, In : Frontiers in Endocrinology. 9, MAY, 17 p., 249.

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Structural insights into binding specificity, efficacy and bias of a β 2 AR partial agonist

Masureel, M., Zou, Y., Picard, L. P., van der Westhuizen, E., Mahoney, J. P., Rodrigues, J. P. G. L. M., Mildorf, T. J., Dror, R. O., Shaw, D. E., Bouvier, M., Pardon, E., Steyaert, J., Sunahara, R. K., Weis, W. I., Zhang, C. & Kobilka, B. K., 1 Nov 2018, In : Nature Chemical Biology. 14, 11, p. 1059-1066 8 p.

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Structure-based discovery of selective positive allosteric modulators of antagonists for the M2 muscarinic acetylcholine receptor

Korczynska, M., Clark, M. J., Valant, C., Xu, J., Moo, E. V., Albold, S., Weiss, D. R., Torosyan, H., Huang, W., Kruse, A. C., Lyda, B. R., May, L. T., Baltos, J. A., Sexton, P. M., Kobilka, B. K., Christopoulos, A., Shoichet, B. K. & Sunahara, R. K., 6 Mar 2018, In : Proceedings of the National Academy of Sciences. 115, 10, p. E2419-E2428 10 p.

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Structure of the adenosine-bound human adenosine A1 receptor-Gi complex

Draper-Joyce, C. J., Khoshouei, M., Thal, D. M., Liang, Y. L., Nguyen, A. T. N., Furness, S. G. B., Venugopal, H., Baltos, J. A., Plitzko, J. M., Danev, R., Baumeister, W., May, L. T., Wootten, D., Sexton, P. M., Glukhova, A. & Christopoulos, A., 20 Jun 2018, In : Nature. 558, 7711, p. 559-565 7 p.

Research output: Contribution to journalArticleResearchpeer-review