Research Output 1986 2019

2018

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.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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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.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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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.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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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.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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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

Open Access
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Endothelial Progenitor Cells and Vascular Health in Dialysis Patients

Huuskes, B. M., DeBuque, R. J., Polkinghorne, K. R., Samuel, C. S., Kerr, P. G. & Ricardo, S. D., Jan 2018, In : Kidney International Reports. 3, 1, p. 205-211 7 p.

Research output: Contribution to journalLetterResearchpeer-review

Open Access
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Evidence that NF-κB and MAPK Signaling Promotes NLRP Inflammasome Activation in Neurons Following Ischemic Stroke

Fann, D. Y. W., Lim, Y. A., Cheng, Y. L., Lok, K. Z., Chunduri, P., Baik, S. H., Drummond, G. R., Dheen, S. T., Sobey, C. G., Jo, D. G., Chen, C. L. H. & Arumugam, T. V., Feb 2018, In : Molecular Neurobiology. 55, 2, p. 1082-1096 15 p.

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

Open Access
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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

Genetically Encoded FRET Biosensors to Illuminate Compartmentalised GPCR Signalling

Halls, M. L. & Canals, M., 1 Feb 2018, In : Trends in Pharmacological Sciences. 39, 2, p. 148-157 10 p.

Research output: Contribution to journalReview ArticleResearchpeer-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

G protein–coupled receptors targeting insulin resistance, obesity, and type 2 diabetes mellitus

Riddy, D. M., Delerive, P., Summers, R. J., Sexton, P. & Langmead, C. J., 1 Jan 2018, In : Pharmacological Reviews. 70, 1, p. 39-67 29 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

Hexarelin treatment preserves myocardial function and reduces cardiac fibrosis in mouse model of acute myocardial infarction

McDonald, H., Peart, J., Kurniawan, N., Galloway, G., Royce, S., Samuel, C. S. & Chen, C., 13 May 2018, In : Physiological Reports. 6, 9, 14 p., e13699.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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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

IL-33 modulates inflammatory brain injury but exacerbates systemic immunosuppression following ischemic stroke

Zhang, S. R., Piepke, M., Chu, H. X., Broughton, B. R. S., Shim, R., Wong, C. H. Y., Lee, S., Evans, M. A., Vinh, A., Sakkal, S., Arumugam, T. V., Magnus, T., Huber, S., Gelderblom, M., Drummond, G. R., Sobey, C. G. & Kim, H. A., 20 Sep 2018, In : JCI Insight. 3, 18, 16 p., e121560.

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

Open Access
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Insights into endotoxin-mediated lung inflammation and future treatment strategies

Chakraborty, A., Boer, J. C., Selomulya, C., Plebanski, M. & Royce, S. G., 2 Nov 2018, In : Expert Review of Respiratory Medicine. 12, 11, p. 941-955 15 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

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.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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Macrophage migration inhibitory factor is required for NLRP3 inflammasome activation

Lang, T., Lee, J. P. W., Elgass, K., Pinar, A. A., Tate, M. D., Aitken, E. H., Fan, H., Creed, S. J., Deen, N. S., Traore, D. A. K., Mueller, I., Stanisic, D., Baiwog, F. S., Skene, C., Wilce, M. C. J., Mansell, A., Morand, E. F. & Harris, J., 1 Dec 2018, In : Nature Communications. 9, 1, 15 p., 2223.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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Mechanisms of signalling and biased agonism in G protein-coupled receptors

Wootten, D. L., Christopoulos, A., Marti-Solano, M., Babu, M. M. & Sexton, P. M., Oct 2018, In : Nature Reviews Molecular Cell Biology. 19, 10, p. 638-653 16 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

Open Access
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Missing Heritability of Hypertension and Our Microbiome: Have we been searching in the wrong place?

Marques, F. Z., 2 Oct 2018, In : Circulation. 138, 14, p. 1381-1383 3 p.

Research output: Contribution to journalEditorialOtherpeer-review

Molecular pharmacology of GPCRs

Langmead, C. J. & Summers, R. J., 1 Nov 2018, In : British Journal of Pharmacology. 175, 21, p. 4005-4008 4 p.

Research output: Contribution to journalEditorialOther

Open Access
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Morphology and function of the lamb ileum following preterm birth

Flores, T. J., Nguyen, V. B., Widdop, R. E., Sutherland, M. R., Polglase, G. R., Abud, H. E. & Black, M. J., 29 Jan 2018, In : Frontiers in Pediatrics. 6, 11 p., 8.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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Multisite phosphorylation is required for sustained interaction with GRKs and arrestins during rapid -opioid receptor desensitization

Miess, E., Gondin, A. B., Yousuf, A., Steinborn, R., Mösslein, N., Yang, Y., Göldner, M., Ruland, J. G., Bünemann, M., Krasel, C., Christie, M. J., Halls, M. L., Schulz, S. & Canals, M., 17 Jul 2018, In : Science Signaling. 11, 539, 15 p., eaas9609.

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.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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New paradigms in adenosine receptor pharmacology: allostery, oligomerization and biased agonism

Vecchio, E. A., Baltos, J. A., Nguyen, A. T. N., Christopoulos, A., White, P. J. & May, L. T., 1 Nov 2018, In : British Journal of Pharmacology. 175, 21, p. 4036-4046 11 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

Non-neurotoxic activity of Malayan krait (Bungarus candidus) venom from Thailand

Charoenpitakchai, M., Wiwatwarayos, K., Jaisupa, N., Rusmili, M. R. A., Mangmool, S., Hodgson, W. C., Ruangpratheep, C., Chanhome, L. & Chaisakul, J., 9 Mar 2018, In : Journal of Venomous Animals and Toxins Including Tropical Diseases. 24, 1, 9 p., 9.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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NOX2 oxidase expressed in endosomes promotes cell proliferation and prostate tumour development

Harrison, I. P., Vinh, A., Johnson, I. R. D., Luong, R., Drummond, G. R., Sobey, C. G., Tiganis, T., Williams, E. D., O'Leary, J., Brooks, D. A. & Selemidis, S., 23 Oct 2018, In : Oncotarget. 9, 83, p. 35378-35393 16 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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Peripheral modulation of the endocannabinoid system in metabolic disease

Shrestha, N., Cuffe, J. S. M., Hutchinson, D. S., Headrick, J. P., Perkins, A. V., McAinch, A. J. & Hryciw, D. H., 1 Mar 2018, In : Drug Discovery Today. 23, 3, p. 592-604 13 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

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.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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Population-Based Gut Microbiome Associations With Hypertension

Jama, H., Kaye, D. M. & Marques, F. Z., 9 Nov 2018, In : Circulation Research. 123, 11, p. 1185-1187 3 p.

Research output: Contribution to journalComment / DebateOtherpeer-review

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.

Research output: Contribution to journalArticleResearchpeer-review

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Probing the binding site of novel selective positive allosteric modulators at the M1 muscarinic acetylcholine receptor

Khajehali, E., Valant, C., Jörg, M., Tobin, A. B., Conn, P. J., Lindsley, C. W., Sexton, P. M., Scammells, P. J. & Christopoulos, A., 1 Aug 2018, In : Biochemical Pharmacology. 154, p. 243-254 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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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 others, Scheff, 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.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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Proteomic Characterization of Two Medically Important Malaysian Snake Venoms, Calloselasma rhodostoma (Malayan Pit Viper) and Ophiophagus hannah (King Cobra)

Kunalan, S., Othman, I., Syed Hassan, S. & Hodgson, W. C., 26 Oct 2018, In : Toxins. 10, 11, 36 p., 434.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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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

Rattling the border wall: Pathophysiological implications of functional and proteomic venom variation between Mexican and US subspecies of the desert rattlesnake Crotalus scutulatus

Dobson, J., Yang, D. C., op den Brouw, B., Cochran, C., Huynh, T., Kurrupu, S., Sánchez, E. E., Massey, D. J., Baumann, K., Jackson, T. N. W., Nouwens, A., Josh, P., Neri-Castro, E., Alagón, A., Hodgson, W. C. & Fry, B. G., 1 Feb 2018, In : Comparative Biochemistry and Physiology Part - C: Toxicology and Pharmacology. 205, p. 62-69 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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Regulation of the human placental (pro)renin receptor-prorenin-angiotensin system by microRNAs

Wang, Y., Lumbers, E. R., Arthurs, A. L., Corbisier de Meaultsart, C., Mathe, A., Avery-Kiejda, K. A., Roberts, C. T., Broughton Pipkin, F., Marques, F. Z., Morris, B. J. & Pringle, K. G., 1 Sep 2018, In : Molecular Human Reproduction. 24, 9, p. 453-464 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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Renal nerves contribute to hypertension in Schlager BPH/2J mice

Gueguen, C., Jackson, K. L., Marques, F. Z., Eikelis, N., Phillips, S., Stevenson, E. R., Charchar, F. J., Lambert, G. W., Davern, P. J. & Head, G. A., 10 Dec 2018, In : Hypertension Research. 42, p. 306-318 13 p.

Research output: Contribution to journalArticleResearchpeer-review