Research Output 1986 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

AT1R-AT2R-RXFP1 functional crosstalk in myofibroblasts: Impact on the therapeutic targeting of renal and cardiac fibrosis

Chow, B. S. M., Kocan, M., Shen, M., Wang, Y., Han, L., Chew, J. Y., Wang, C., Bosnyak, S., Mirabito-Colafella, K. M., Barsha, G., Wigg, B., Johnstone, E. K. M., Hossain, M. A., Pfleger, K. D. G., Denton, K. M., Widdop, R. E., Summers, R. J., Bathgate, R. A. D., Hewitson, T. D. & Samuel, C. S., Sep 2019, (Accepted/In press) In : Journal of the American Society of Nephrology. 30, 9, 18 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., 1 Oct 2019, In : Journal of Medicinal Chemistry. 62, 1, p. 174-206 33 p.

Research output: Contribution to journalArticleResearchpeer-review

Atypical cannabinoid ligands O-1602 and O-1918 administered chronically in diet-induced obesity

Simcocks, A. C., Jenkin, K. A., O’Keefe, L., Samuel, C. S., Mathai, M. L., McAinch, A. J. & Hryciw, D. H., Mar 2019, In : Endocrine Connections. 8, 3, p. 203-216 14 p.

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BRL37344 stimulates GLUT4 translocation and glucose uptake in skeletal muscle via β 2 -adrenoceptors without causing classical receptor desensitization

Mukaida, S., Sato, M., Öberg, A. I., Dehvari, N., Olsen, J. M., Kocan, M., Halls, M. L., Merlin, J., Sandström, A. L., Csikasz, R. I., Evans, B. A., Summers, R. J., Hutchinson, D. S. & Bengtsson, T., 1 May 2019, In : American journal of physiology. Regulatory, integrative and comparative physiology. 316, 5, p. R666-R677 12 p.

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Cardioprotective actions of the annexin-A1 N-terminal peptide, AC2-26, against myocardial infarction

Qin, C. X., Rosli, S., Deo, M., Cao, N., Walsh, J., Tate, M., Alexander, A. E., Donner, D., Horlock, D., Li, R., Kiriazis, H., Lee, M. K. S., Bourke, J. E., Yang, Y., Murphy, A. J., Du, X-J., Gao, X. M. & Ritchie, R. H., 3 Apr 2019, In : Frontiers in Pharmacology. 10, 16 p., 269.

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Chronic sympathetic driven hypertension promotes atherosclerosis by enhancing hematopoiesis

Al-Sharea, A., Lee, M. K. S., Whillas, A., Michell, D. L., Shihata, W. A., Nicholls, A. J., Cooney, O. D., Kraakman, M. J., Veiga, C. B., Jefferis, A. M., Jackson, K., Nagareddy, P. R., Lambert, G., Wong, C. H. Y., Andrews, K. L., Head, G. A., Chin-Dusting, J. & Murphy, A. J., 28 Feb 2019, In : Haematologica: the hematology journal. 104, 3, p. 456-467 12 p.

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D. Russelii venom mediates vasodilatation of resistance like arteries via activation of k v and k ca channels

Kakumanu, R., Kuruppu, S., Rash, L. D., Isbister, G. K., Hodgson, W. C. & Kemp-Harper, B. K., 1 Apr 2019, In : Toxins. 11, 4, 10 p., 197.

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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.

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Effects of high- and low-dose aspirin on adaptive immunity and hypertension in the stroke-prone spontaneously hypertensive rat

Khan, S. I., Shihata, W. A., Andrews, K. L., Lee, M. K. S., Moore, X-L., Jefferis, A-M., Vinh, A., Gaspari, T., Dragoljevic, D., Jennings, G. L., Murphy, A. J. & Chin-Dusting, J. P. F., 1 Jan 2019, In : FASEB Journal. 33, 1, p. 1510-1521 12 p.

Research output: Contribution to journalArticleResearchpeer-review

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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Glycine microparticles loaded with functionalized nanoparticles for pulmonary delivery

Chakraborty, A., Royce, S. G., Plebanski, M. & Selomulya, C., 30 Oct 2019, In : International Journal of Pharmaceutics. 570, 9 p., 118654.

Research output: Contribution to journalArticleResearchpeer-review

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.

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Human amnion epithelial cells and their soluble factors reduce liver fibrosis in murine non-alcoholic steatohepatitis

Kuk, N., Hodge, A., Sun, Y., Correia, J., Alhomrani, M., Samuel, C., Moore, G., Lim, R. & Sievert, W., Aug 2019, In : Journal of Gastroenterology and Hepatology (Australia). 34, 8, p. 1441-1449 9 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

IL-37 increases in patients after ischemic stroke and protects from inflammatory brain injury, motor impairment and lung infection in mice

Zhang, S. R., Nold, M. F., Tang, S. C., Bui, C. B., Nold, C. A., Arumugam, T. V., Drummond, G. R., Sobey, C. G. & Kim, H. A., 1 Dec 2019, In : Scientific Reports. 9, 1, 12 p., 6922.

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Interleukin-1 receptor antagonist protects newborn mice against pulmonary hypertension

Bui, C. B., Kolodziej, M., Lamanna, E., Elgass, K., Sehgal, A., Rudloff, I., Schwenke, D. O., Tsuchimochi, H., Kroon, M. A. G. M., Cho, S. X., Maksimenko, A., Cholewa, M., Berger, P. J., Young, M. J., Bourke, J. E., Pearson, J. T., Nold, M. F. & Nold-Petry, C. A., 11 Jul 2019, In : Frontiers in Immunology. 10, JULY, 15 p., 1480.

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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

NOx in exhaled breath condensate is related to allergic sensitization in young and middle-aged adults

Aldakheel, F. M., Bourke, J. E., Thomas, P. S., Matheson, M. C., Abramson, M. J., Hamilton, G. S., Lodge, C. J., Thompson, B. R., Haydn Walters, E., Allen, K. J., Erbas, B., Perret, J. L., Dharmage, S. C. & Lowe, A. J., Feb 2019, In : Clinical and Experimental Allergy. 49, 2, p. 171-179 9 p.

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Pharmacological inhibition of the NLRP3 inflammasome reduces blood pressure, renal damage, and dysfunction in salt-sensitive hypertension

Krishnan, S. M., Ling, Y. H., Huuskes, B. M., Ferens, D. M., Saini, N., Chan, C. T., Diep, H., Kett, M. M., Samuel, C. S., Kemp-Harper, B. K., Robertson, A. A. B., Cooper, M. A., Peter, K., Latz, E., Mansell, A. S., Sobey, C. G., Drummond, G. R. & Vinh, A., 15 Mar 2019, In : Cardiovascular Research. 115, 4, p. 776-787 12 p.

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Profiling histone modifications in the normal mouse kidney and after unilateral ureteric obstruction

Hewitson, T. D., Holt, S. G., Samuel, C. S., Wigg, B. & Smith, E. R., 1 Sep 2019, In : American journal of physiology. Renal physiology. 317, 3, p. F606-F615 10 p.

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Serelaxin enhances the therapeutic effects of human amnion epithelial cell-derived exosomes in experimental models of lung disease

Royce, S. G., Patel, K. P., Mao, W., Zhu, D., Lim, R. & Samuel, C. S., Jul 2019, In : British Journal of Pharmacology. 176, 13, p. 2195-2208 14 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 gut microbiota and blood pressure in experimental models

Jama, H. A., Kaye, D. M. & Marques, F. Z., 1 Mar 2019, In : Current Opinion in Nephrology and Hypertension. 28, 2, p. 97-104 8 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 use of live cell imaging and automated image analysis to assist with determining optimal parameters for angiogenic assay in vitro

Huuskes, B. M., DeBuque, R. J., Kerr, P. G., Samuel, C. S. & Ricardo, S. D., 10 Apr 2019, In : Frontiers in Cell and Developmental Biology. 7, 14 p., 45.

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Vampire venom: Vasodilatory mechanisms of vampire bat (desmodus rotundus) blood feeding

Kakumanu, R., Hodgson, W. C., Ravi, R., Alagon, A., Harris, R. J., Brust, A., Alewood, P. F., Kemp-Harper, B. K. & Fry, B. G., 8 Jan 2019, In : Toxins. 11, 1, 10 p., 26.

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2018

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 others, Selemidis, 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

Age-related differential structural and transcriptomic responses in the hypertensive heart

Marques, F. Z., Chu, P. Y., Ziemann, M., Kaspi, A., Kiriazis, H., Du, X. J., El-Osta, A. & Kaye, D. M., 9 Jul 2018, In : Frontiers in Physiology. 9, JUL, 13 p., 817.

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A polymorphism in the noradrenaline transporter gene is associated with increased blood pressure in patients with resistant hypertension

Eikelis, N., Marques, F. Z., Hering, D., Marusic, P., Head, G. A., Walton, A. S., Lambert, E. A., Esler, M. D., Sari, C. I., Schlaich, M. P. & Lambert, G. W., 1 Jul 2018, In : Journal of Hypertension. 36, 7, p. 1571-1577 7 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

Circadian differences in the contribution of the brain renin-angiotensin system in genetically hypertensive mice

Jackson, K. L., Marques, F. Z., Lim, K., Davern, P. J. & Head, G. A., 19 Mar 2018, In : Frontiers in Physiology. 9, 15 p., 231.

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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

Dapagliflozin attenuates human vascular endothelial cell activation and induces vasorelaxation: A potential mechanism for inhibition of atherogenesis

Gaspari, T., Spizzo, I., Liu, H., Hu, Y., Simpson, R. W., Widdop, R. E. & Dear, A. E., 1 Jan 2018, In : Diabetes and Vascular Disease Research. 15, 1, p. 64-73 10 p.

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Defective cholesterol metabolism in haematopoietic stem cells promotes monocyte-driven atherosclerosis in rheumatoid arthritis

Dragoljevic, D., Kraakman, M. J., Nagareddy, P. R., Ngo, D., Shihata, W., Kammoun, H. L., Whillas, A., Lee, M. K. S., Al-Sharea, A., Pernes, G., Flynn, M. C., Lancaster, G. I., Febbraio, M. A., Chin-Dusting, J., Hanaoka, B. Y., Wicks, I. P. & Murphy, A. J., 14 Jun 2018, In : European Heart Journal. 39, 23, p. 2158-2167 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Defining the role of post-synaptic α-neurotoxins in paralysis due to snake envenoming in humans

Silva, A., Cristofori-Armstrong, B., Rash, L. D., Hodgson, W. C. & Isbister, G. K., 1 Dec 2018, In : Cellular and Molecular Life Sciences. 75, 23, p. 4465-4478 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Diet-induced vitamin D deficiency has no effect on acute post-stroke outcomes in young male mice

Evans, M. A., Kim, H. A., De Silva, T. M., Arumugam, T. V., Clarkson, A. N., Drummond, G. R., Zosky, G. R., Broughton, B. R. S. & Sobey, C. G., 1 Nov 2018, In : Journal of Cerebral Blood Flow and Metabolism. 38, 11, p. 1968-1978 11 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

Divergent effects of strontium and calcium-sensing receptor positive allosteric modulators (calcimimetics) on human osteoclast activity

Diepenhorst, N. A., Leach, K., Keller, A. N., Rueda, P., Cook, A. E., Pierce, T. L., Nowell, C., Pastoureau, P., Sabatini, M., Summers, R. J., Charman, W. N., Sexton, P. M., Christopoulos, A. & Langmead, C. J., 1 Nov 2018, In : British Journal of Pharmacology. 175, 21, p. 4095-4108 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Dual Action Calcium-Sensing Receptor Modulator Unmasks Novel Mode-Switching Mechanism

Gregory, K., Kufareva, I., Keller, A. N., Khajehali, E., Mun, H., Goolam, M. A., Mason, R. S., Capuano, B., Conigrave, A., Christopoulos, A. & Leach, K., 12 Sep 2018, In : ACS Pharmacology and Translational Sciences. 1, 2, p. 96-109 14 p.

Research output: Contribution to journalArticleResearchpeer-review

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