R
Romain Luc Marie Gosmini
Researcher at GlaxoSmithKline
Publications - 13
Citations - 1255
Romain Luc Marie Gosmini is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Bromodomain & Allosteric modulator. The author has an hindex of 7, co-authored 13 publications receiving 1087 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.
Journal ArticleDOI
Bet Inhibition Silences Expression of Mycn and Bcl2 and Induces Cytotoxicity in Neuroblastoma Tumor Models.
Anastasia Wyce,Gopinath Ganji,Kimberly N. Smitheman,Chun-wa Chung,Susan Korenchuk,Yuchen Bai,Olena Barbash,BaoChau Le,Peter D. Craggs,Michael T. McCabe,Karen M. Kennedy-Wilson,Lydia V. Sanchez,Romain Luc Marie Gosmini,Nigel J. Parr,Charles F. McHugh,Dashyant Dhanak,Rab K. Prinjha,Kurt R. Auger,Peter J. Tummino +18 more
TL;DR: Evidence is provided for potent BET inhibitor activity in neuroblastoma, a pediatric solid tumor associated with a high frequency of MYCN amplifications, and a role of BET inhibition in apoptosis, signaling, and N-Myc-driven pathways, including the direct suppression of BCL2 and MYCN is suggested.
Journal ArticleDOI
The Discovery of I-BET726 (GSK1324726A), a Potent Tetrahydroquinoline ApoA1 Up-Regulator and Selective BET Bromodomain Inhibitor
Romain Luc Marie Gosmini,Van Loc Nguyen,Jérôme Toum,Christophe Simon,Jean-Marie Brusq,Gael Krysa,Olivier Mirguet,Alizon M. Riou-Eymard,Eric Boursier,Lionel Trottet,Paul Bamborough,Hugh Clark,Chun-wa Chung,Leanne Cutler,Emmanuel Hubert Demont,Rejbinder Kaur,Antonia J. Lewis,Mark B. Schilling,Peter Ernest Soden,Simon Taylor,Ann Louise Walker,Matthew D. Walker,Rab K. Prinjha,Edwige Nicodeme +23 more
TL;DR: This work describes the identification of a novel tetrahydroquinoline series through up-regulation of apolipoprotein A1 and the optimization into potent compounds active in murine models of septic shock and neuroblastoma, and reveals the interactions explaining the structure-activity relationships of binding.
Journal ArticleDOI
From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151.
Olivier Mirguet,Yann Lamotte,Frédéric Donche,Jérôme Toum,Françoise Gellibert,Anne Marie Jeanne Bouillot,Romain Luc Marie Gosmini,Van-Loc Nguyen,Delphine Delannée,Jonathan Thomas Seal,Florence Blandel,Anne-Benedicte Boullay,Eric Boursier,Sandrine Martin,Jean-Marie Brusq,Gael Krysa,Alizon M. Riou,Rémi Tellier,Agnès Costaz,Pascal Huet,Yann Dudit,Lionel Trottet,Jorge Kirilovsky,Edwige Nicodeme +23 more
TL;DR: The discovery, synthesis and biological evaluation of a novel series of 7-isoxazoloquinolines is described and several analogs are shown to increase ApoA1 expression within the nanomolar range in the human hepatitis cell line HepG2.