Search Results - "Webster, Scott P"

Mass Spectrometry Imaging for Dissecting Steroid Intracrinology within Target Tissues by Cobice, Diego F, Mackay, C. Logan, Goodwin, Richard J. A, McBride, Andrew, Langridge-Smith, Patrick R, Webster, Scott P, Walker, Brian R, Andrew, Ruth

“…Steroid concentrations within tissues are modulated by intracellular enzymes. Such “steroid intracrinology” influences hormone-dependent cancers and obesity…”
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Kynurenine 3-monooxygenase is a critical regulator of renal ischemia–reperfusion injury by Zheng, Xiaozhong, Zhang, Ailiang, Binnie, Margaret, McGuire, Kris, Webster, Scott P., Hughes, Jeremy, Howie, Sarah E. M., Mole, Damian J.

“…Acute kidney injury (AKI) following ischemia–reperfusion injury (IRI) has a high mortality and lacks specific therapies. Here, we report that mice lacking…”
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Structural and mechanistic basis of differentiated inhibitors of the acute pancreatitis target kynurenine-3-monooxygenase by Hutchinson, Jonathan P., Rowland, Paul, Taylor, Mark R. D., Christodoulou, Erica M., Haslam, Carl, Hobbs, Clare I., Holmes, Duncan S., Homes, Paul, Liddle, John, Mole, Damian J., Uings, Iain, Walker, Ann L., Webster, Scott P., Mowat, Christopher G., Chung, Chun-wa

“…Kynurenine-3-monooxygenase (KMO) is a key FAD-dependent enzyme of tryptophan metabolism. In animal models, KMO inhibition has shown benefit in…”
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11β-HSD1 inhibition does not affect murine tumour angiogenesis but may exert a selective effect on tumour growth by modulating inflammation and fibrosis by Davidson, Callam T, Miller, Eileen, Muir, Morwenna, Dawson, John C, Lee, Martin, Aitken, Stuart, Serrels, Alan, Webster, Scott P, Homer, Natalie Z M, Andrew, Ruth, Brunton, Valerie G, Hadoke, Patrick W F, Walker, Brian R

“…Glucocorticoids inhibit angiogenesis by activating the glucocorticoid receptor. Inhibition of the glucocorticoid-activating enzyme 11β-hydroxysteroid…”
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Fast acting allosteric phosphofructokinase inhibitors block trypanosome glycolysis and cure acute African trypanosomiasis in mice by McNae, Iain W., Kinkead, James, Malik, Divya, Yen, Li-Hsuan, Walker, Martin K., Swain, Chris, Webster, Scott P., Gray, Nick, Fernandes, Peter M., Myburgh, Elmarie, Blackburn, Elizabeth A., Ritchie, Ryan, Austin, Carol, Wear, Martin A., Highton, Adrian J., Keats, Andrew J., Vong, Antonio, Dornan, Jacqueline, Mottram, Jeremy C., Michels, Paul A. M., Pettit, Simon, Walkinshaw, Malcolm D.

“…The parasitic protist Trypanosoma brucei is the causative agent of Human African Trypanosomiasis, also known as sleeping sickness. The parasite enters the…”
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Kynurenine monooxygenase regulates inflammation during critical illness and recovery in experimental acute pancreatitis by Hayes, Alastair J., Zheng, Xiaozhong, O’Kelly, James, Neyton, Lucile P.A., Bochkina, Natalia A., Uings, Iain, Liddle, John, Baillie, J. Kenneth, Just, George, Binnie, Margaret, Homer, Natalie Z.M., Murray, Toby B.J., Baily, James, McGuire, Kris, Skouras, Christos, Garden, O. James, Webster, Scott P., Iredale, John P., Howie, Sarah E.M., Mole, Damian J.

“…Kynurenine monooxygenase (KMO) blockade protects against multiple organ failure caused by acute pancreatitis (AP), but the link between KMO and systemic…”
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11β-Hydroxysteroid Dehydrogenase Type 1 Is Expressed in Neutrophils and Restrains an Inflammatory Response in Male Mice by Coutinho, Agnes E, Kipari, Tiina M. J, Zhang, Zhenguang, Esteves, Cristina L, Lucas, Christopher D, Gilmour, James S, Webster, Scott P, Walker, Brian R, Hughes, Jeremy, Savill, John S, Seckl, Jonathan R, Rossi, Adriano G, Chapman, Karen E

“…Endogenous glucocorticoid action within cells is enhanced by prereceptor metabolism by 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), which converts…”
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Exploring N-acyl-4-azatetracyclo[5.3.2.0 2,6 .0 8,10 ]dodec-11-enes as 11β-HSD1 Inhibitors by Leiva, Rosana, McBride, Andrew, Binnie, Margaret, Webster, Scott P, Vázquez, Santiago

“…We recently found that a cyclohexanecarboxamide derived from 4-azatetracyclo[5.3.2.0 .0 ]dodec-11-ene displayed low nanomolar inhibition of 11β-HSD1. In…”
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Increased levels of 3-hydroxykynurenine parallel disease severity in human acute pancreatitis by Skouras, Christos, Zheng, Xiaozhong, Binnie, Margaret, Homer, Natalie Z. M., Murray, Toby B. J., Robertson, Darren, Briody, Lesley, Paterson, Finny, Spence, Heather, Derr, Lisa, Hayes, Alastair J., Tsoumanis, Andreas, Lyster, Dawn, Parks, Rowan W., Garden, O. James, Iredale, John P., Uings, Iain J., Liddle, John, Wright, Wayne L., Dukes, George, Webster, Scott P., Mole, Damian J.

“…Inhibition of kynurenine 3-monooxygenase (KMO) protects against multiple organ dysfunction (MODS) in experimental acute pancreatitis (AP). We aimed to…”
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UFSRAT: Ultra-fast Shape Recognition with Atom Types--the discovery of novel bioactive small molecular scaffolds for FKBP12 and 11βHSD1 by Shave, Steven, Blackburn, Elizabeth A, Adie, Jillian, Houston, Douglas R, Auer, Manfred, Webster, Scott P, Taylor, Paul, Walkinshaw, Malcolm D

“…Using molecular similarity to discover bioactive small molecules with novel chemical scaffolds can be computationally demanding. We describe Ultra-fast Shape…”
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Elevated hepatic 11β-hydroxysteroid dehydrogenase type 1 induces insulin resistance in uremia by Chapagain, Ananda, Caton, Paul W., Kieswich, Julius, Andrikopoulos, Petros, Nayuni, Nanda, Long, Jamie H., Harwood, Steven M., Webster, Scott P., Raftery, Martin J., Thiemermann, Christoph, Walker, Brian R., Seckl, Jonathan R., Corder, Roger, Yaqoob, Muhammad Magdi

“…Insulin resistance and associated metabolic sequelae are common in chronic kidney disease (CKD) and are positively and independently associated with increased…”
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Diclofenac Identified as a Kynurenine 3‑Monooxygenase Binder and Inhibitor by Molecular Similarity Techniques by Shave, Steven, McGuire, Kris, Pham, Nhan T, Mole, Damian J, Webster, Scott P, Auer, Manfred

“…In this study, we apply a battery of molecular similarity techniques to known inhibitors of kynurenine 3-monooxygenase (KMO), querying each against a…”
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β-Cell-Specific Glucocorticoid Reactivation Attenuates Inflammatory β-Cell Destruction by Liu, Xiaoxia, Turban, Sophie, Carter, Roderick N, Ahmad, Shakil, Ramage, Lynne, Webster, Scott P, Walker, Brian R, Seckl, Jonathan R, Morton, Nicholas M

“…Progression and severity of type 1 diabetes is dependent upon inflammatory induction of nitric oxide production and consequent pancreatic β-cell damage…”
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Kynurenine-3-monooxygenase inhibition prevents multiple organ failure in rodent models of acute pancreatitis by Mole, Damian J, Webster, Scott P, Uings, Iain, Zheng, Xiaozhong, Binnie, Margaret, Wilson, Kris, Hutchinson, Jonathan P, Mirguet, Olivier, Walker, Ann, Beaufils, Benjamin, Ancellin, Nicolas, Trottet, Lionel, Bénéton, Véronique, Mowat, Christopher G, Wilkinson, Martin, Rowland, Paul, Haslam, Carl, McBride, Andrew, Homer, Natalie Z M, Baily, James E, Sharp, Matthew G F, Garden, O James, Hughes, Jeremy, Howie, Sarah E M, Holmes, Duncan S, Liddle, John, Iredale, John P

“…Blocking the enzyme KMO with a small molecule reduces the levels of toxic tryptophan metabolites and reduces multiple extrapancreatic organ failure in a rat…”
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Cognitive and Disease-Modifying Effects of 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibition in Male Tg2576 Mice, a Model of Alzheimer's Disease by Sooy, Karen, Noble, June, McBride, Andrew, Binnie, Margaret, Yau, Joyce L. W, Seckl, Jonathan R, Walker, Brian R, Webster, Scott P

“…Chronic exposure to elevated levels of glucocorticoids has been linked to age-related cognitive decline and may play a role in Alzheimer's disease. In the…”
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Vitamin A deficiency impairs contextual fear memory in rats: Abnormalities in the glucocorticoid pathway by Bonhomme, Damien, Alfos, Serge, Webster, Scott P., Wolff, Mathieu, Pallet, Véronique, Touyarot, Katia

“…Vitamin A and its active metabolite, retinoic acid (RA), play a key role in the maintenance of cognitive functions in the adult brain. Depletion of RA using…”
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Memory deficits in a juvenile rat model of type 1 diabetes are due to excess 11β-HSD1 activity, which is upregulated by high glucose concentrations rather than insulin deficiency by Brossaud, Julie, Bosch-Bouju, Clémentine, Marissal-Arvy, Nathalie, Campas-Lebecque, Marie-Neige, Helbling, Jean-Christophe, Webster, Scott P., Walker, Brian R., Fioramonti, Xavier, Ferreira, Guillaume, Barat, Pascal, Corcuff, Jean-Benoît, Moisan, Marie-Pierre

“…Aims/hypothesis Children with diabetes may display cognitive alterations although vascular disorders have not yet appeared. Variations in glucose levels…”
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Mechanism of 8-Amino-7-oxononanoate Synthase:  Spectroscopic, Kinetic, and Crystallographic Studies by Webster, Scott P, Alexeev, Dmitriy, Campopiano, Dominic J, Watt, Rory M, Alexeeva, Marina, Sawyer, Lindsay, Baxter, Robert L

“…8-Amino-7-oxononanoate synthase (also known as 7-keto-8-aminopelargonate synthase, EC 2.3.1.47) is a pyridoxal 5‘-phosphate-dependent enzyme which catalyzes…”
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Rapid Discovery and Structure–Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase by Fraser, Craig, Dawson, John C, Dowling, Reece, Houston, Douglas R, Weiss, Jason T, Munro, Alison F, Muir, Morwenna, Harrington, Lea, Webster, Scott P, Frame, Margaret C, Brunton, Valerie G, Patton, E. Elizabeth, Carragher, Neil O, Unciti-Broceta, Asier

“…Novel pyrazolopyrimidines displaying high potency and selectivity toward SRC family kinases have been developed by combining ligand-based design and phenotypic…”
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Selection and early clinical evaluation of the brain‐penetrant 11β‐hydroxysteroid dehydrogenase type 1 (11β‐HSD1) inhibitor UE2343 (Xanamem™) by Webster, Scott P, McBride, Andrew, Binnie, Margaret, Sooy, Karen, Seckl, Jonathan R, Andrew, Ruth, Pallin, T David, Hunt, Hazel J, Perrior, Trevor R, Ruffles, Vincent S, Ketelbey, J William, Boyd, Alan, Walker, Brian R

“…Background and Purpose Reducing glucocorticoid exposure in the brain via intracellular inhibition of the cortisol‐regenerating enzyme 11β‐hydroxysteroid…”
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