J
John Liddle
Researcher at GlaxoSmithKline
Publications - 83
Citations - 2501
John Liddle is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Oxytocin receptor & Syk. The author has an hindex of 20, co-authored 83 publications receiving 2112 citations. Previous affiliations of John Liddle include University of East Anglia & Loughborough University.
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Journal ArticleDOI
A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response
Laurens Kruidenier,Chun-wa Chung,Zhongjun Cheng,John Liddle,K.H. Che,K.H. Che,Gerard Joberty,Marcus Bantscheff,C. Bountra,Angela Bridges,Hawa Diallo,Dirk Eberhard,Sue Hutchinson,Emma J. Jones,Roy Katso,Melanie Leveridge,Palwinder K. Mander,J. Mosley,Cesar Ramirez-Molina,Paul Rowland,Christopher J. Schofield,Robert J. Sheppard,Julia Smith,Catherine Swales,Robert Tanner,Pamela Thomas,Anthony Tumber,Gerard Drewes,Udo Oppermann,Udo Oppermann,Dinshaw J. Patel,Kevin Lee,Kevin Lee,David Matthew Wilson +33 more
TL;DR: It is demonstrated that the first small-molecule catalytic site inhibitor that is selective for the H3K27me3-specific JMJ subfamily binds in a novel manner and reduces lipopolysaccharide-induced proinflammatory cytokine production by human primary macrophages, a process that depends on both JMJD3 and UTX.
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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.
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Kynurenine-3-monooxygenase inhibition prevents multiple organ failure in rodent models of acute pancreatitis
Damian J. Mole,Scott P. Webster,Iain Uings,Xiaozhong Zheng,Margaret Binnie,Kris Wilson,Jonathan P. Hutchinson,Olivier Mirguet,Ann Louise Walker,Benjamin Beaufils,Nicolas Ancellin,Lionel Trottet,Veronique Beneton,Christopher G. Mowat,Martin Wilkinson,Paul Rowland,Carl Haslam,Andrew McBride,Natalie Z.M. Homer,James Baily,Matthew G.F. Sharp,O. James Garden,Jeremy Hughes,Sarah E. M. Howie,Duncan S. Holmes,John Liddle,John P. Iredale +26 more
TL;DR: It is shown that kynurenine-3-monooxygenase (KMO), a key enzyme of tryptophan metabolism, is central to the pathogenesis of AP-MODS and it is established KMO inhibition as a novel therapeutic strategy in the treatment of AP.
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The discovery of GSK221149A: A potent and selective oxytocin antagonist
John Liddle,Michael Allen,Alan D. Borthwick,David P. Brooks,David E. Davies,Richard M. Edwards,Anne M. Exall,Christopher Charles Frederick Hamlett,Wendy R. Irving,Andrew M. Mason,Gerald P. McCafferty,Fabrizio Nerozzi,Simon Peace,Joanne Philp,Derek Pollard,Mark Pullen,Shaila S. Shabbir,Steve L. Sollis,Timothy D. Westfall,Pat M. Woollard,Charlene Wu,Deirdre Mary Bernadette Hickey +21 more
TL;DR: Optimisation of a series of oxazole diketopiperazines has led to the discovery of a very potent and selective oxytocin antagonist GSK221149A, which has been shown to inhibit oxytocarine contractions in the anaesthetised rat.
Journal ArticleDOI
Pyridyl-2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists: synthesis, pharmacokinetics, and in vivo potency.
Alan D. Borthwick,John Liddle,Dave E. Davies,Anne M. Exall,Christopher Charles Frederick Hamlett,Deirdre Mary Bernadette Hickey,Andrew M. Mason,Ian Edward David Smith,Fabrizio Nerozzi,Simon Peace,Derek Pollard,Steve L. Sollis,Michael Allen,Patrick M. Woollard,Mark Pullen,Timothy D. Westfall,Dinesh Stanislaus +16 more
TL;DR: Epelsiban has low levels of intrinsic clearance against the microsomes of four species, good bioavailability and comparable potency to atosiban in the rat, but is 100-fold more potent than the latter in vitro and was negative in the genotoxicity screens with a satisfactory oral safety profile in female rats.