Search Results - "Bayle, D."

New approaches for the treatment of Alzheimer’s disease by Fish, Paul V., Steadman, David, Bayle, Elliott D., Whiting, Paul

“…[Display omitted] Alzheimer’s disease (AD) is the most prevalent chronic neurodegenerative disease. Current approved therapies are symptomatic treatments…”
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Copper-Catalyzed Electrophilic Carbofunctionalization of Alkynes to Highly Functionalized Tetrasubstituted Alkenes by Suero, Marcos G, Bayle, Elliott D, Collins, Beatrice S. L, Gaunt, Matthew J

“…Copper catalysts enable the electrophilic carbofunctionalization of alkynes with vinyl- and diaryliodonium triflates. The new process forms highly substituted…”
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Systematic Investigation of the Permeability of Androgen Receptor PROTACs by Scott, Duncan E, Rooney, Timothy P. C, Bayle, Elliott D, Mirza, Tashfina, Willems, Henriette M. G, Clarke, Jonathan H, Andrews, Stephen P, Skidmore, John

“…Bifunctional molecules known as PROTACs simultaneously bind an E3 ligase and a protein of interest to direct ubiquitination and clearance of that protein, and…”
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Design of a Chemical Probe for the Bromodomain and Plant Homeodomain Finger-Containing (BRPF) Family of Proteins by Igoe, Niall, Bayle, Elliott D, Tallant, Cynthia, Fedorov, Oleg, Meier, Julia C, Savitsky, Pavel, Rogers, Catherine, Morias, Yannick, Scholze, Sarah, Boyd, Helen, Cunoosamy, Danen, Andrews, David M, Cheasty, Anne, Brennan, Paul E, Müller, Susanne, Knapp, Stefan, Fish, Paul V

“…The bromodomain and plant homeodomain finger-containing (BRPF) family are scaffolding proteins important for the recruitment of histone acetyltransferases of…”
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An improved, scalable synthesis of Notum inhibitor LP-922056 using 1-chloro-1,2-benziodoxol-3-one as a superior electrophilic chlorinating agent by Willis, Nicky J, Bayle, Elliott D, Papageorgiou, George, Steadman, David, Atkinson, Benjamin N, Mahy, William, Fish, Paul V

“…The carboxylesterase Notum has been shown to act as a key negative regulator of the Wnt signalling pathway by mediating the depalmitoleoylation of Wnt…”
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What Value Can Operational Feasibility Studies Bring to Post Marketing Observational Studies (PMOS)? Example of Feasibility Study Performed in Eastern Europe to Assess Hepatitis C Viral Disease/Patient Management in Real World Setting by El Kebir, S, Bayle, D, Gauchoux, R

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Cortical dynamics of externally and self-directed attention: a MEG study of a card sorting task by Fonlupt, P., Henaff, M.A., Bayle, D., Krolak-Salmon, P.

“…Introduction Neuroimaging studies using functional magnetic resonance imaging (fMRI) have revealed different neural networks within the frontal cortex dealing…”
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Carboxylesterase Notum Is a Druggable Target to Modulate Wnt Signaling by Bayle, Elliott D, Svensson, Fredrik, Atkinson, Benjamin N, Steadman, David, Willis, Nicky J, Woodward, Hannah L, Whiting, Paul, Vincent, Jean-Paul, Fish, Paul V

“…Regulation of the Wnt signaling pathway is critically important for a number of cellular processes in both development and adult mammalian biology. This…”
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New small molecule inhibitors of histone methyl transferase DOT1L with a nitrile as a non-traditional replacement for heavy halogen atoms by Spurr, Sophie S., Bayle, Elliott D., Yu, Wenyu, Li, Fengling, Tempel, Wolfram, Vedadi, Masoud, Schapira, Matthieu, Fish, Paul V.

“…[Display omitted] A number of new nucleoside derivatives are disclosed as inhibitors of DOT1L activity. SARs established that DOT1L inhibition could be…”
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Design of a Potent, Selective, and Brain-Penetrant Inhibitor of Wnt-Deactivating Enzyme Notum by Optimization of a Crystallographic Fragment Hit by Willis, Nicky J., Mahy, William, Sipthorp, James, Zhao, Yuguang, Woodward, Hannah L., Atkinson, Benjamin N., Bayle, Elliott D., Svensson, Fredrik, Frew, Sarah, Jeganathan, Fiona, Monaghan, Amy, Benvegnù, Stefano, Jolly, Sarah, Vecchia, Luca, Ruza, Reinis R., Kjær, Svend, Howell, Steven, Snijders, Ambrosius P., Bictash, Magda, Salinas, Patricia C., Vincent, Jean-Paul, Jones, E. Yvonne, Whiting, Paul, Fish, Paul V.

“…Notum is a carboxylesterase that suppresses Wnt signaling through deacylation of an essential palmitoleate group on Wnt proteins. There is a growing…”
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Inhibitory effect of procyanidin-rich extracts on LDL oxidation in vitro by Mazur, A, Bayle, D, Lab, C, Rock, E, Rayssiguier, Y

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Scaffold-hopping identifies furano[2,3-d]pyrimidine amides as potent Notum inhibitors by Atkinson, Benjamin N., Steadman, David, Mahy, William, Zhao, Yuguang, Sipthorp, James, Bayle, Elliott D., Svensson, Fredrik, Papageorgiou, George, Jeganathan, Fiona, Frew, Sarah, Monaghan, Amy, Bictash, Magda, Jones, E. Yvonne, Fish, Paul V.

“…[Display omitted] The carboxylesterase Notum is a key negative regulator of the Wnt signaling pathway by mediating the depalmitoleoylation of Wnt proteins. Our…”
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Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies by Igoe, Niall, Bayle, Elliott D, Fedorov, Oleg, Tallant, Cynthia, Savitsky, Pavel, Rogers, Catherine, Owen, Dafydd R, Deb, Gauri, Somervaille, Tim C. P, Andrews, David M, Jones, Neil, Cheasty, Anne, Ryder, Hamish, Brennan, Paul E, Müller, Susanne, Knapp, Stefan, Fish, Paul V

“…The BRPF (bromodomain and PHD finger-containing) family are scaffolding proteins important for the recruitment of histone acetyltransferases of the MYST family…”
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Morphological and immune response alterations in the intestinal mucosa of the mouse after short periods on a low-magnesium diet by Zimowska, W., Girardeau, J. P., Kuryszko, J., Bayle, D., Rayssiguier, Y., Mazur, A.

“…The importance of Mg for the immune function is well recognized; however, there is no information available about the effect of Mg intake on the modulation of…”
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Physical exercise influences attentional orientation towards emotional stimuli by Mansouri, N., Coutté, A., Dru, V., Bayle, D.

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Structural Analysis and Development of Notum Fragment Screening Hits by Zhao, Yuguang, Mahy, William, Willis, Nicky J, Woodward, Hannah L, Steadman, David, Bayle, Elliott D, Atkinson, Benjamin N, Sipthorp, James, Vecchia, Luca, Ruza, Reinis R, Harlos, Karl, Jeganathan, Fiona, Constantinou, Stefan, Costa, Artur, Kjær, Svend, Bictash, Magda, Salinas, Patricia C, Whiting, Paul, Vincent, Jean-Paul, Fish, Paul V, Jones, E Yvonne

“…The Wnt signaling suppressor Notum is a promising target for osteoporosis, Alzheimer's disease, and colorectal cancers. To develop novel Notum inhibitors, we…”
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Selective Targeting of Bromodomains of the Bromodomain-PHD Fingers Family Impairs Osteoclast Differentiation by Meier, Julia C, Tallant, Cynthia, Fedorov, Oleg, Witwicka, Hanna, Hwang, Sung-Yong, van Stiphout, Ruud G, Lambert, Jean-Philippe, Rogers, Catherine, Yapp, Clarence, Gerstenberger, Brian S, Fedele, Vita, Savitsky, Pavel, Heidenreich, David, Daniels, Danette L, Owen, Dafydd R, Fish, Paul V, Igoe, Niall M, Bayle, Elliott D, Haendler, Bernard, Oppermann, Udo C.T, Buffa, Francesca, Brennan, Paul E, Müller, Susanne, Gingras, Anne Claude, Odgren, Paul R, Birnbaum, Mark J, Knapp, Stefan

“…Histone acetyltransferases of the MYST family are recruited to chromatin by BRPF scaffolding proteins. We explored functional consequences and the therapeutic…”
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Changes in gene expression in the lungs of Mg-deficient mice are related to an inflammatory process by NASULEWICZ, A, ZIMOWSKA, W, BAYLE, D, DZIMIRA, S, MADEJ, J, RAYSSIGUIER, Y, OPOLSKI, A, MAZUR, A

“…It has been well documented that experimental hypomagnesemia in rodents evokes, as an early consequence, an inflammatory response. This also leads to the…”
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Effects of Ionizing Radiation (Neutrons/Gamma Rays) on Plasma Lipids and Lipoproteins in Rats by Feurgard, C., Bayle, D., Guézingar, F., Sérougne, C., Mazur, A., Lutton, C., Aigueperse, J., Gourmelon, P., Mathé, D.

“…Male Wistar rats weighing 250 g were exposed to 4 Gy of neutrons/γ radiation (3.33 Gy of neutrons and 0.66 Gy of γ rays). After whole-body irradiation, plasma…”
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Response of diamine oxidase and other plasma copper biomarkers to various dietary copper intakes in the rat and evaluation of copper absorption with a stable isotope by Feillet-Coudray, C., Coudray, C., Bayle, D., Rock, E., Rayssiguier, Y., Mazur, A.

“…There is a lack of agreement on index of Cu status and reliable and sensitive biomarkers are still required. The purpose of this present work was to assess in…”
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