P
Paul Bamborough
Researcher at GlaxoSmithKline
Publications - 89
Citations - 4676
Paul Bamborough is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Bromodomain & Kinase. The author has an hindex of 33, co-authored 86 publications receiving 3998 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
Comprehensive characterization of the Published Kinase Inhibitor Set
Jonathan M. Elkins,Vita Fedele,M. Szklarz,Kamal R. Abdul Azeez,Eidarus Salah,Jowita Mikolajczyk,Sergei Romanov,Nikolai Sepetov,Xi Ping Huang,Bryan L. Roth,Ayman Al Haj Zen,Denis Fourches,Eugene N. Muratov,Alexander Tropsha,Joel Morris,Beverly A. Teicher,Mark Kunkel,Eric C. Polley,Karen Lackey,Francis Atkinson,John P. Overington,John P. Overington,Paul Bamborough,Susanne Müller,Daniel J. Price,Timothy M. Willson,Timothy M. Willson,David H. Drewry,David H. Drewry,Stefan Knapp,Stefan Knapp,William J. Zuercher,William J. Zuercher +32 more
TL;DR: A thorough characterization of the Published Kinase Inhibitor Set is provided and chemical starting points for designing new chemical probes of orphan kinases are identified and the utility of these leads are illustrated by developing a selective inhibitor for the previously untargeted kinases LOK and SLK.
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.
Journal ArticleDOI
Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson's disease
R. Jeremy Nichols,Nicolas Dzamko,Jessica E. Hutti,Jessica E. Hutti,Lewis C. Cantley,Lewis C. Cantley,Maria Deak,Jennifer Moran,Paul Bamborough,Alastair D. Reith,Dario R. Alessi +10 more
TL;DR: A pharmacological approach to validate whether substrates are phosphorylated by LRRK2 and use this to provide evidence that L RRK2 may not be rate-limiting for the phosphorylation of the proposed substrate moesin is described.