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Iain Uings
Researcher at GlaxoSmithKline
Publications - 39
Citations - 1889
Iain Uings is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Glucocorticoid receptor & Agonist. The author has an hindex of 20, co-authored 39 publications receiving 1693 citations.
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Journal ArticleDOI
Discovery and Characterization of Small Molecule Inhibitors of the Bet Family Bromodomains.
Chun-wa Chung,Hervé Coste,Julia H. White,Olivier Mirguet,Jonathan I. Wilde,Romain Luc Marie Gosmini,Chris J. Delves,Sylvie M. Magny,Robert Woodward,Stephen A. Hughes,Eric Boursier,Helen R. Flynn,Anne Marie Jeanne Bouillot,Paul Bamborough,Jean-Marie Brusq,Françoise Gellibert,Emma J. Jones,Alizon M. Riou,Paul Homes,Sandrine Martin,Iain Uings,Jérôme Toum,Catherine A. Clément,Anne-Benedicte Boullay,Rachel Grimley,Florence Blandel,Rab K. Prinjha,Kevin Lee,Jorge Kirilovsky,Edwige Nicodeme +29 more
TL;DR: X-ray crystal structures of compounds bound into bromodomains of Brd2 and Brd4 elucidate the molecular interactions of binding and explain the precisely defined stereochemistry required for activity.
Journal ArticleDOI
Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains
Olivier Mirguet,Romain Luc Marie Gosmini,Jérôme Toum,Catherine A. Clément,Mélanie Barnathan,Jean-Marie Brusq,Jacqueline Elizabeth Mordaunt,Grimes Richard Martin,Miriam Crowe,Olivier Pineau,Myriam Ajakane,Alain Claude-Marie Daugan,Phillip Jeffrey,Leanne Cutler,Andrea C. Haynes,Nicholas Smithers,Chun-wa Chung,Paul Bamborough,Iain Uings,Antonia J. Lewis,Jason Witherington,Nigel J. Parr,Rab K. Prinjha,Edwige Nicodeme +23 more
TL;DR: This work has yielded a potent, selective compound I-BET762 that is now under evaluation in a phase I/II clinical trial for nuclear protein in testis (NUT) midline carcinoma and other cancers.
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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.
Mark Salter,Keith Biggadike,Joyce Lesley Matthews,Michael Robert West,Michael V. Haase,Stuart N. Farrow,Iain Uings,David W. Gray +7 more
TL;DR: The potent and selective pharmacological profile of FF described here could deliver an effective, safe, and sustained topical treatment of respiratory inflammatory diseases such as allergic rhinitis and asthma.
Journal ArticleDOI
Kynurenine-3-monooxygenase inhibition prevents multiple organ failure in rodent models of acute pancreatitis
Damian J. Mole,Scott P. Webster,Iain Uings,Xiaozhong Zheng,Margaret Binnie,Kris Wilson,Jonathan P. Hutchinson,Olivier Mirguet,Ann Louise Walker,Benjamin Beaufils,Nicolas Ancellin,Lionel Trottet,Veronique Beneton,Christopher G. Mowat,Martin Wilkinson,Paul Rowland,Carl Haslam,Andrew McBride,Natalie Z.M. Homer,James Baily,Matthew G.F. Sharp,O. James Garden,Jeremy Hughes,Sarah E. M. Howie,Duncan S. Holmes,John Liddle,John P. Iredale +26 more
TL;DR: It is shown that kynurenine-3-monooxygenase (KMO), a key enzyme of tryptophan metabolism, is central to the pathogenesis of AP-MODS and it is established KMO inhibition as a novel therapeutic strategy in the treatment of AP.
Journal ArticleDOI
Glucocorticoid-induced osteopenia in the mouse as assessed by histomorphometry, microcomputed tomography, and biochemical markers.
F. McLaughlin,J. Mackintosh,Brian Hayes,A. McLaren,Iain Uings,P. Salmon,J. Humphreys,E. Meldrum,Stuart N. Farrow +8 more
TL;DR: B/c mice represent a useful model system in which the detrimental effects of glucocorticoids on bone can be studied, and serum levels of leptin, recently identified as playing a role in the regulation of bone mass, increased following dexamethasone treatment.