Search Results - "Uings, Iain J"

Discovery of Epigenetic Regulator I‑BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains by Mirguet, Olivier, Gosmini, Romain, Toum, Jérôme, Clément, Catherine A, Barnathan, Mélanie, Brusq, Jean-Marie, Mordaunt, Jacqueline E, Grimes, Richard M, Crowe, Miriam, Pineau, Olivier, Ajakane, Myriam, Daugan, Alain, Jeffrey, Phillip, Cutler, Leanne, Haynes, Andrea C, Smithers, Nicholas N, Chung, Chun-wa, Bamborough, Paul, Uings, Iain J, Lewis, Antonia, Witherington, Jason, Parr, Nigel, Prinjha, Rab K, Nicodème, Edwige

“…The bromo and extra C-terminal domain (BET) family of bromodomains are involved in binding epigenetic marks on histone proteins, more specifically acetylated…”
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Pharmacological properties of the enhanced-affinity glucocorticoid fluticasone furoate in vitro and in an in vivo model of respiratory inflammatory disease by Salter, Mark, Biggadike, Keith, Matthews, Joyce L, West, Michael R, Haase, Michael V, Farrow, Stuart N, Uings, Iain J, Gray, David W

“…Fluticasone furoate (FF) is a novel enhanced-affinity glucocorticoid that has been developed as topical therapy for allergic rhinitis. The pharmacological…”
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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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Design and x-ray crystal structures of high-potency nonsteroidal glucocorticoid agonists exploiting a novel binding site on the receptor by Biggadike, Keith, Bledsoe, Randy K, Coe, Diane M, Cooper, Tony W.J, House, David, Iannone, Marie A, Macdonald, Simon J.F, Madauss, Kevin P, McLay, Iain M, Shipley, Tracy J, Taylor, Simon J, Tran, Thuy B, Uings, Iain J, Weller, Victoria, Williams, Shawn P

“…Crystallography and computer modeling have been used to exploit a previously unexplored channel in the glucocorticoid receptor (GR). Highly potent,…”
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Discovery and Characterization of Small Molecule Inhibitors of the BET Family Bromodomains by Chung, Chun-wa, Coste, Hervé, White, Julia H, Mirguet, Olivier, Wilde, Jonathan, Gosmini, Romain L, Delves, Chris, Magny, Sylvie M, Woodward, Robert, Hughes, Stephen A, Boursier, Eric V, Flynn, Helen, Bouillot, Anne M, Bamborough, Paul, Brusq, Jean-Marie G, Gellibert, Françoise J, Jones, Emma J, Riou, Alizon M, Homes, Paul, Martin, Sandrine L, Uings, Iain J, Toum, Jérôme, Clément, Catherine A, Boullay, Anne-Bénédicte, Grimley, Rachel L, Blandel, Florence M, Prinjha, Rab K, Lee, Kevin, Kirilovsky, Jorge, Nicodeme, Edwige

“…Epigenetic mechanisms of gene regulation have a profound role in normal development and disease processes. An integral part of this mechanism occurs through…”
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The discovery of potent and selective kynurenine 3-monooxygenase inhibitors for the treatment of acute pancreatitis by Liddle, John, Beaufils, Benjamin, Binnie, Margaret, Bouillot, Anne, Denis, Alexis A., Hann, Michael M., Haslam, Carl P., Holmes, Duncan S., Hutchinson, Jon P., Kranz, Michael, McBride, Andrew, Mirguet, Olivier, Mole, Damian J., Mowat, Christopher G., Pal, Sandeep, Rowland, Paul, Trottet, Lionel, Uings, Iain J., Walker, Ann L., Webster, Scott P.

“…[Display omitted] A series of potent, competitive and highly selective kynurenine monooxygenase inhibitors have been discovered via a substrate-based approach…”
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The first X-ray crystal structure of the glucocorticoid receptor bound to a non-steroidal agonist by MADAUSS, Kevin P, BLEDSOE, Randy K, MCLAY, Iain, STEWART, Eugene L, UINGS, Iain J, WEINGARTEN, Gordon, WILLIAMS, Shawn P

“…The amino-pyrazole 2,6-dichloro-N-ethyl benzamide 1 is a selective GR agonist with dexamethasone-like in vitro potency. Its X-ray crystal structure in the GR…”
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Structure Guided Design of 5-Arylindazole Glucocorticoid Receptor Agonists and Antagonists by Yates, Christopher M, Brown, Peter J, Stewart, Eugene L, Patten, Christopher, Austin, Robert J. H, Holt, Jason A, Maglich, Jodi M, Angell, Davina C, Sasse, Rosemary Z, Taylor, Simon J, Uings, Iain J, Trump, Ryan P

“…Glucocorticoid receptor (GR) agonists have been used for more than half a century as the most effective treatment of acute and chronic inflammatory conditions…”
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Cytokine-Specific Transcriptional Regulation through an IL-5Rα Interacting Protein by Geijsen, Niels, Uings, Iain J., Pals, Cornelieke, Armstrong, John, McKinnon, Murray, Jan A. M. Raaijmakers, Lammers, Jan-Willem J., Koenderman, Leo, Coffer, Paul J.

“…Cytokine receptors consist of multiple subunits, which are often shared between different receptors, resulting in the functional redundancy sometimes observed…”
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Discovery of a potent series of non-steroidal non α-trifluoromethyl carbinol glucocorticoid receptor agonists with reduced lipophilicity by Diallo, Hawa, Angell, Davina C., Barnett, Heather A., Biggadike, Keith, Coe, Diane M., Cooper, Tony W.J., Craven, Andy, Gray, James R., House, David, Jack, Torquil I., Keeling, Steve P., Macdonald, Simon J.F., McLay, Iain M., Oliver, Samuel, Taylor, Simon J., Uings, Iain J., Wellaway, Natalie

“…A novel series of indazole non-steroidal glucocorticoid receptor agonist has been discovered. This series features a sulfonamide central core and meta amides…”
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Aryl aminopyrazole benzamides as oral non-steroidal selective glucocorticoid receptor agonists by Barnett, Heather A., Coe, Diane M., Cooper, Tony W.J., Jack, Torquil I., Jones, Haydn T., Macdonald, Simon J.F., McLay, Iain M., Rayner, Natalie, Sasse, Rosemary Z., Shipley, Tracy J., Skone, Phil A., Somers, Graham I., Taylor, Simon, Uings, Iain J., Woolven, James M., Weingarten, Gordon G.

“…SAR leading to the oral selective non-steroidal GR agonist 16e is described. Aryl aminopyrazole amides capped with N-alkylbenzamides 13– 16 are selective…”
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A pharmacological approach to enhancing the therapeutic index of corticosteroids in airway inflammatory disease by Uings, Iain J, Farrow, Stuart N

“…Inhaled corticosteroids are highly effective agents for the treatment of asthma and chronic obstructive pulmonary disease. Although local delivery to the lung…”
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Inhibition of nuclear factor‐κB activation un‐masks the ability of TNF‐α to induce human eosinophil apoptosis by Fujihara, Satoko, Ward, Carol, Dransfield, Ian, Hay, Ronald T., Uings, Iain J., Hayes, Brian, Farrow, Stuart N., Haslett, Christopher, Rossi, Adriano G.

“…Apoptosis renders eosinophils functionally effete and marks them for ‘silent’ removal from inflamed sites by macrophages. We show, for the first time, that…”
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Functional analysis of the interleukin-5 receptor antagonist peptide, AF18748 by Rosas, Marcela, Uings, Iain J, van Aalst, Cornelli, Lammers, Jan-Willem J, Koenderman, Leo, Coffer, Paul J

“…AF18748 is a dimeric peptide of 2×19 amino acids that specifically binds to the α-chain of the human IL-5 receptor (IL-5R), preventing binding of IL-5 and…”
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An interleukin 5 mutant distinguishes between two functional responses in human eosinophils by McKinnon, M, Page, K, Uings, I J, Banks, M, Fattah, D, Proudfoot, A E, Graber, P, Arod, C, Fish, R, Wells, T N, Solari, R

“…Interleukin 5 (IL-5) is the key cytokine involved in regulating the production and many of the specialized functions of mature eosinophils including priming,…”
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Indolocarbazoles: Potent and Selective Inhibitors of Platelet-Derived Growth Factor Receptor Autophosphorylation by Spacey, Graham D, Uings, Iain J, Slater, Martin, Hirst, Stuart, Bonser, Robert W

“…A quantitative assay for measuring the autophosphorylation of platelet-derived growth factor (PDGF) receptors in intact vascular smooth muscle cells has been…”
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Functional analysis of the interleukin-1-receptor-associated kinase (IRAK-1) in interleukin-1 beta-stimulated nuclear factor kappa B (NF-kappa B) pathway activation: IRAK-1 associates with the NF-kappa B essential modulator (NEMO) upon receptor stimulation by Cooke, E L, Uings, I J, Xia, C L, Woo, P, Ray, K P

“…The interleukin-1 (IL-1)-receptor-associated kinase (IRAK-1) is essential for IL-1-stimulated nuclear factor kappa B (NF-kappa B) activation. To study the role…”
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Functional analysis of the interleukin-1-receptor-associated kinase (IRAK-1) in interleukin-1β-stimulated nuclear factor κB (NF-κB) pathway activation: IRAK-1 associates with the NF-κB essential modulator (NEMO) upon receptor stimulation by COOKE, Emma-Louise, UINGS, Iain J., XIA, Chulin L., WOO, Patricia, RAY, Keith P.

“…The interleukin-1 (IL-1)-receptor-associated kinase (IRAK-1) is essential for IL-1-stimulated nuclear factor κB (NF-κB) activation. To study the role of IRAK-1…”
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Inhibition of nuclear factor-kappaB activation un-masks the ability of TNF-alpha to induce human eosinophil apoptosis by Fujihara, Satoko, Ward, Carol, Dransfield, Ian, Hay, Ronald T, Uings, Iain J, Hayes, Brian, Farrow, Stuart N, Haslett, Christopher, Rossi, Adriano G

“…Apoptosis renders eosinophils functionally effete and marks them for "silent" removal from inflamed sites by macrophages. We show, for the first time, that…”
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Cytokine-Specific Transcriptional Regulation Through an IL-5R[Alpha] Interacting Protein by Geijsen, Niels, Uings, Iain J, Pals, Cornelieke, Armstrong, John, McKinnon, Murray, Raaijmakers, Jan A. M, Lammers, Jan-Willem J, Koenderman, Leo, Coffer, Paul J

“…Cytokine receptors consist of multiple subunits, which are often shared between different receptors, resulting in the functional redundancy sometimes observed…”
Get full text