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Edwige Nicodeme
Researcher at GlaxoSmithKline
Publications - 24
Citations - 3370
Edwige Nicodeme is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Bromodomain & BRD4. The author has an hindex of 18, co-authored 24 publications receiving 2990 citations.
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Journal ArticleDOI
Suppression of inflammation by a synthetic histone mimic
Edwige Nicodeme,Kate L. Jeffrey,Uwe Schaefer,Soren Beinke,Scott Dewell,Chun-wa Chung,Rohit Chandwani,Ivan Marazzi,Paul A. Wilson,Hervé Coste,Julia H. White,Jorge Kirilovsky,Charles M. Rice,Jose M. Lora,Rab K. Prinjha,Kevin Lee,Alexander Tarakhovsky +16 more
TL;DR: A synthetic compound (I-BET) is described that by ‘mimicking’ acetylated histones disrupts chromatin complexes responsible for the expression of key inflammatory genes in activated macrophages, and confers protection against lipopolysaccharide-induced endotoxic shock and bacteria-induced sepsis.
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.
Journal ArticleDOI
Identification of a Novel Series of Bet Family Bromodomain Inhibitors: Binding Mode and Profile of I-Bet151 (Gsk1210151A).
Jonathan Thomas Seal,Yann Lamotte,Frédéric Donche,Anne Marie Jeanne Bouillot,Olivier Mirguet,Françoise Gellibert,Edwige Nicodeme,Gael Krysa,Jorge Kirilovsky,Soren Beinke,Scott McCleary,Inma Rioja,Paul Bamborough,Chun-wa Chung,Laurie J. Gordon,Toni Lewis,Ann Louise Walker,Leanne Cutler,Dave Lugo,David Matthew Wilson,Jason Witherington,Kevin Lee,Rab K. Prinjha +22 more
TL;DR: A novel series of quinoline isoxazole BET family bromodomain inhibitors shows good oral bioavailability in both the rat and minipig as well as demonstrating efficient suppression of bacterial induced inflammation and sepsis in a murine in vivo endotoxaemia model.
Journal ArticleDOI
Tapinarof Is a Natural AhR Agonist that Resolves Skin Inflammation in Mice and Humans
Susan H. Smith,Channa K Jayawickreme,David J. Rickard,Edwige Nicodeme,Thi Bui,Cathy Simmons,Christine M. Coquery,Jessica Neil,William M. Pryor,David L. Mayhew,Deepak K. Rajpal,Katrina L. Creech,Sylvia Furst,James Lee,Dalei Wu,Fraydoon Rastinejad,Timothy M. Willson,Fabrice Viviani,David C. Morris,John T. Moore,Javier Cote-Sierra +20 more
TL;DR: These studies identify tapinarof as an AhR agonist and confirm that its efficacy is dependent on AhR.