R
Rebecca C. Furze
Researcher at GlaxoSmithKline
Publications - 14
Citations - 694
Rebecca C. Furze is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Bromodomain & Inflammation. The author has an hindex of 9, co-authored 14 publications receiving 585 citations.
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Journal ArticleDOI
Broadly Neutralizing Antibodies and Viral Inducers Decrease Rebound from HIV-1 Latent Reservoirs in Humanized Mice
Ariel Halper-Stromberg,Ching-Lan Lu,Florian Klein,Joshua A. Horwitz,Stylianos Bournazos,Lillian Nogueira,Thomas Eisenreich,Cassie Liu,Anna Gazumyan,Uwe Schaefer,Rebecca C. Furze,Michael S. Seaman,Rab K. Prinjha,Alexander Tarakhovsky,Jeffrey V. Ravetch,Michel C. Nussenzweig,Michel C. Nussenzweig +16 more
TL;DR: It is shown that broadly neutralizing antibodies (bNAbs) can interfere with establishment of a silent reservoir by Fc-FcR-mediated mechanisms, and combinations of inducers and bNAbs constitute a therapeutic strategy that impacts the establishment and maintenance of the HIV-1 reservoir in humanized mice.
Journal ArticleDOI
Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors.
Paul Bamborough,Chun-wa Chung,Rebecca C. Furze,Paola Grandi,Anne-Marie Michon,Robert J. Sheppard,Heather A. Barnett,Hawa Diallo,David P. Dixon,Clement Douault,Emma J. Jones,Bhumika Karamshi,Darren Jason Mitchell,Rab K. Prinjha,Christina Rau,Robert J. Watson,Thilo Werner,Emmanuel Hubert Demont +17 more
TL;DR: This article describes the structure-based optimization of a series of naphthyridones from micromolar leads with no selectivity over the BET bromodomains to inhibitors with sub-100 nM ATAD2 potency and 100-fold BET selectivity.
Journal ArticleDOI
Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors
Emmanuel Hubert Demont,Chun-wa Chung,Rebecca C. Furze,Paola Grandi,Anne-Marie Michon,Christopher Roland Wellaway,Nathalie Barrett,Angela Bridges,Peter D. Craggs,Hawa Diallo,David P. Dixon,Clement Douault,Amanda Emmons,Emma J. Jones,Bhumika Karamshi,Kelly Locke,Darren Jason Mitchell,Bernadette Mouzon,Rab K. Prinjha,Andrew D. Roberts,Robert J. Sheppard,Robert J. Watson,Paul Bamborough +22 more
TL;DR: The discovery of a hit from a fragment-based targeted array is described, which produced the first known micromolar inhibitors of the ATAD2 bromodomain.
Journal ArticleDOI
A Chemical Probe for the ATAD2 Bromodomain
Paul Bamborough,Chun-wa Chung,Emmanuel Hubert Demont,Rebecca C. Furze,Andrew J. Bannister,Ka Hing Che,Hawa Diallo,Clement Douault,Paola Grandi,Tony Kouzarides,Anne-Marie Michon,Darren Jason Mitchell,Rab K. Prinjha,Christina Rau,Samuel Robson,Robert J. Sheppard,Robert J. Sheppard,Richard J. Upton,Robert J. Watson +18 more
TL;DR: This work reports the first reported low-nanomolar, selective and cell permeable chemical probe for ATAD2, a cancer-associated protein whose bromodomain has been described as among the least druggable of that target class.
Journal ArticleDOI
The structure based design of dual HDAC/BET inhibitors as novel epigenetic probes
Stephen John Atkinson,Peter Ernest Soden,Davina C. Angell,Marcus Bantscheff,Chun-wa Chung,Kathryn A. Giblin,Nicholas Smithers,Rebecca C. Furze,Laurie J. Gordon,Gerard Drewes,Inmaculada Rioja,Jason Witherington,Nigel J. Parr,Rab K. Prinjha +13 more
TL;DR: The design and synthesis of a dual active histone deacetylase (HDAC)/bromodomain and extra terminal (BET) small molecule tool inhibitor, DUAL946 is described, which was confirmed by in vitro biochemical and biophysical testing and through chemoproteomic competition experiments in cell lysates.