S
Stephen John Atkinson
Researcher at GlaxoSmithKline
Publications - 42
Citations - 1421
Stephen John Atkinson is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Bromodomain & Histone deacetylase. The author has an hindex of 14, co-authored 41 publications receiving 1014 citations.
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Journal ArticleDOI
Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation
Huw D. Lewis,John Liddle,Jim E Coote,Stephen John Atkinson,Michael David Barker,Benjamin D. Bax,Kevin L. Bicker,Ryan P. Bingham,Matthew Campbell,Yu Hua Chen,Chun-wa Chung,Peter D. Craggs,Robert P. Davis,Dirk Eberhard,Gerard Joberty,Kenneth E Lind,Kelly Locke,Claire Maller,Kimberly Martinod,Chris Patten,Oxana Polyakova,Cecil E Rise,Martin Rüdiger,Robert J. Sheppard,Daniel J. Slade,Pamela Thomas,Jim Thorpe,Gang Yao,Gerard Drewes,Denisa D. Wagner,Paul R. Thompson,Rab K. Prinjha,David Matthew Wilson +32 more
TL;DR: Novel, selective PAD4 inhibitors binding to a calcium-deficient form of the PAD3 enzyme have been validated, for the first time, in both histone citrullination and neutrophil extracellular trap formation, validating the critical enzymatic role of human and mouse PAD 4.
Journal ArticleDOI
Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation
Omer Gilan,Omer Gilan,Inmaculada Rioja,Kathy Knezevic,Matthew J Bell,Miriam M. Yeung,Nicola Harker,Enid Y.N. Lam,Enid Y.N. Lam,Chun-wa Chung,Paul Bamborough,Massimo Petretich,Marjeta Urh,Stephen John Atkinson,Anna K. Bassil,Emma J. Roberts,Dane Vassiliadis,Dane Vassiliadis,Marian L. Burr,Marian L. Burr,Alex Preston,Christopher Roland Wellaway,Thilo Werner,James Gray,Anne Marie Michon,Thomas Gobbetti,Vinod Kumar,Peter Ernest Soden,Andrea C. Haynes,Johanna Vappiani,David F. Tough,Simon Taylor,Sarah-Jane Dawson,Sarah-Jane Dawson,Marcus Bantscheff,Matthew J Lindon,Gerard Drewes,Emmanuel Hubert Demont,Danette L. Daniels,Paola Grandi,Rab K. Prinjha,Mark A. Dawson,Mark A. Dawson +42 more
TL;DR: It is found that steady-state gene expression primarily requires BD1, whereas the rapid increase of gene expression induced by inflammatory stimuli requires both BD1 and BD2 of all BET proteins, which may guide future BET-targeted therapies.
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Chan–Evans–Lam Amination of Boronic Acid Pinacol (BPin) Esters: Overcoming the Aryl Amine Problem
Julien C. Vantourout,Robert P. Law,Albert Isidro-Llobet,Stephen John Atkinson,Allan J. B. Watson +4 more
TL;DR: A mixed MeCN/EtOH solvent system was found to enable effective C-N bond formation using aryl amines while EtOH is not required for the coupling of alkyl amine.
Journal ArticleDOI
Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain
Robert P. Law,Stephen John Atkinson,Paul Bamborough,Chun-wa Chung,Emmanuel Hubert Demont,Laurie J. Gordon,Matthew J Lindon,Rab K. Prinjha,Allan J. B. Watson,David Jonathan Hirst +9 more
TL;DR: Focused library screening identified a series of tetrahydroquinoxalines with selectivity for the second bromodomains of the BET family (BD2), culminating in potent BET inhibitors with BD2 selectivity.
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.