Research Output 1969 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.

Research output: Contribution to journalArticleResearchpeer-review

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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., 1 Oct 2019, In : Journal of Medicinal Chemistry. 62, 1, p. 174-206 33 p.

Research output: Contribution to journalArticleResearchpeer-review

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

Development of a shape-controlled H 2 S delivery system using epoxide-functional nanoparticles

Yu, S. H., Esser, L., Khor, S. Y., Senyschyn, D., Veldhuis, N. A., Whittaker, M. R., Ercole, F., Davis, T. P. & Quinn, J. F., 23 Apr 2019, (Accepted/In press) In : Journal of Polymer Science, Part A: Polymer Chemistry. 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Direct Comparison of Standard Transmission Electron Microscopy and Cryogenic-TEM in Imaging Nanocrystals Inside Liposomes

Li, T., Nowell, C. J., Cipolla, D., Rades, T. & Boyd, B. J., 1 Apr 2019, In : Molecular Pharmaceutics. 16, 4, p. 1775-1781 7 p.

Research output: Contribution to journalArticleResearchpeer-review

Drug-receptor kinetics and sigma-1 receptor affinity differentiate clinically evaluated histamine H3 receptor antagonists

Riddy, D. M., Cook, A. E., Shackleford, D. M., Pierce, T. L., Mocaer, E., Mannoury la Cour, C., Sors, A., Charman, W. N., Summers, R. J., Sexton, P. M., Christopoulos, A. & Langmead, C. J., 1 Jan 2019, In : Neuropharmacology. 144, p. 244-255 12 p.

Research output: Contribution to journalArticleResearchpeer-review

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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.

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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

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

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

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

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

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., 11 Jan 2019, In : ACS Pharmacology and Translational Sciences. 2, 1, p. 31-51 21 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.

Research output: Contribution to journalArticleResearchpeer-review

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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.

Research output: Contribution to journalArticleResearchpeer-review

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

Bitopic binding mode of an M1 muscarinic acetylcholine receptor agonist associated with adverse clinical trial outcomes S

Bradley, S. J., Molloy, C., Bundgaard, C., Mogg, A. J., Thompson, K. J., Dwomoh, L., Sanger, H. E., Crabtree, M. D., Brooke, S. M., Sexton, P. M., Felder, C. C., Christopoulos, A., Broad, L. M., Tobin, A. B. & Langmead, C. J., 1 Jun 2018, In : Molecular Pharmacology. 93, 6, p. 645-656 12 p.

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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., May 2018, In : Brain, Behavior, and Immunity. 70, p. 36-47 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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Cryo-EM structure of the active, Gs-protein complexed, human CGRP receptor

Liang, Y-L., Khoshouei, M., Deganutti, G., Glukhova, A., Koole, C., Peat, T. S., Radjainia, M., Plitzko, J. M., Baumeister, W., Miller, L. J., Hay, D. L., Christopoulos, A., Reynolds, C. A., Wootten, D. & Sexton, P. M., 27 Sep 2018, In : Nature. 561, 7724, p. 492-497 6 p.

Research output: Contribution to journalArticleResearchpeer-review

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

Discovery and Optimization of Potent and CNS Penetrant M5-Preferring Positive Allosteric Modulators Derived from a Novel, Chiral N-(Indanyl)piperidine Amide Scaffold

Bender, A. M., Cho, H. P., Nance, K. D., Lingenfelter, K. S., Luscombe, V. B., Gentry, P. R., Voigtritter, K., Berizzi, A. E., Sexton, P. M., Langmead, C. J., Christopoulos, A., Locuson, C. W., Bridges, T. M., Chang, S., O'Neill, J. C., Zhan, X., Niswender, C. M., Jones, C. K., Conn, P. J. & Lindsley, C. W., 18 Jul 2018, In : ACS Chemical Neuroscience. 9, 7, p. 1572-1581 10 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

Effects of hypoxia-ischemia and inotropes on expression of cardiac adrenoceptors in the preterm fetal sheep

Hutchinson, D. S., Brew, N., Vu, T., Merlin, J., Hale, N., Walker, D. W. & Wong, F. Y., 1 Nov 2018, In : Journal of Applied Physiology. 125, 5, p. 1368-1377 10 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.

Research output: Contribution to journalArticleResearchpeer-review

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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.

Research output: Contribution to journalArticleResearchpeer-review

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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

Linker chemistry dictates the delivery of a phototoxic organometallic rhenium(i) complex to human cervical cancer cells from core crosslinked star polymer nanoparticles

Yu, S. H., Patra, M., Ferrari, S., Ramirez Garcia, P., Veldhuis, N. A., Kaminskas, L. M., Graham, B., Quinn, J. F., Whittaker, M. R., Gasser, G. & Davis, T. P., 29 Oct 2018, In : Journal of Materials Chemistry B. 6, 47, p. 7805-7810 6 p.

Research output: Contribution to journalArticleResearchpeer-review

LMP2 immunoproteasome promotes lymphocyte survival by degrading apoptotic BH3-only proteins

Zanker, D., Pang, K., Oveissi, S., Lu, C., Faou, P., Nowell, C., Mbogo, G. W., Carotta, S., Quillici, C., Karupiah, G., Hibbs, M. L., Nutt, S. L., Neeson, P., Puthalakath, H. & Chen, W., 1 Oct 2018, In : Immunology and Cell Biology. 96, 9, p. 981-993 13 p.

Research output: Contribution to journalArticleResearchpeer-review

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