Publications by authors named "Huw D Lewis"

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Phenotype-Led Identification of IL-10 Upregulators in Human CD4 T-cells and Elucidation of Their Pharmacology as Highly Selective CDK8/CDK19 Inhibitors.
Simon Nicolle, Mike Barker, John Barrett, Matthew Campbell, Justyna Wojno-Picon, Huw D Lewis

J Med Chem· January 2025

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Phase 1 and preclinical profiling of ESM-HDAC391, a myeloid-targeted histone deacetylase inhibitor, shows enhanced pharmacology and monocytopaenia.
Rebecca C Furze, Judit Molnar, Nigel J Parr, Faiz Ahmad, Yvette Henry, Huw D Lewis

Br J Clin Pharmacol· December 2022

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Carboxylesterase-1 Assisted Targeting of HDAC Inhibitors to Mononuclear Myeloid Cells in Inflammatory Bowel Disease.
Ahmed M I Elfiky, Mohammed Ghiboub, Andrew Y F Li Yim, Ishtu L Hageman, Jan Verhoeff, Huw D Lewis

J Crohns Colitis· May 2022

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Preclinical models of arthritis for studying immunotherapy and immune tolerance.
Gavin R Meehan, Ranjeny Thomas, Shaima Al Khabouri, Pascale Wehr, Catharien Mu Hilkens, Huw D Lewis

Ann Rheum Dis· October 2021

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Novel Insights Into Rheumatoid Arthritis Through Characterization of Concordant Changes in DNA Methylation and Gene Expression in Synovial Biopsies of Patients With Differing Numbers of Swollen Joints.
Andrew Y F Li Yim, Enrico Ferrero, Klio Maratou, Huw D Lewis, George Royal

Front Immunol· September 2021

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BRD4 methylation by the methyltransferase SETD6 regulates selective transcription to control mRNA translation.
Zlata Vershinin, Michal Feldman, Thilo Werner, Lital Estrella Weil, Margarita Kublanovsky, Huw D Lewis

Sci Adv· May 2021

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Targeting Histone Deacetylases in Myeloid Cells Inhibits Their Maturation and Inflammatory Function With Limited Effects on Atherosclerosis.
Rosario Luque-Martin, Jan Van den Bossche, Rebecca C Furze, Annette E Neele, Saskia van der Velden, Huw D Lewis

Front Pharmacol· October 2019

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Optimisation of a novel series of potent and orally bioavailable azanaphthyridine SYK inhibitors.
Neil S Garton, Michael D Barker, Rob P Davis, Clement Douault, Edward Hooper-Greenhill, Huw D Lewis

Bioorg Med Chem Lett· October 2016

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iPAD or PADi-'tablets' with therapeutic disease potential?
Huw D Lewis, Mariana Nacht

Curr Opin Chem Biol· August 2016

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Protein arginine deiminase 2 binds calcium in an ordered fashion: implications for inhibitor design.
Daniel J Slade, Pengfei Fang, Christina J Dreyton, Ying Zhang, Jakob Fuhrmann, Huw D Lewis

ACS Chem Biol· April 2015

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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 J Atkinson, Michael D Barker

Nat Chem Biol· March 2015

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Epigenetic pathway targets for the treatment of disease: accelerating progress in the development of pharmacological tools: IUPHAR Review 11.
David F Tough, Huw D Lewis, Inmaculada Rioja, Matthew J Lindon, Rab K Prinjha

Br J Pharmacol· November 2014

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Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.
John Liddle, Francis L Atkinson, Michael D Barker, Paul S Carter, Neil R Curtis, Huw D Lewis

Bioorg Med Chem Lett· October 2011

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Gamma-secretase-dependent cleavage of amyloid precursor protein regulates osteoblast behavior.
Jane McLeod, Neil Curtis, Huw D Lewis, Mark A Good, Michael J Fagan

FASEB J· September 2009

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Novel orally bioavailable gamma-secretase inhibitors with excellent in vivo activity.
Linda E Keown, Ian Collins, Laura C Cooper, Timothy Harrison, Andrew Madin, Huw D Lewis

J Med Chem· June 2009

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Progression and variability of TNBS colitis-associated inflammation in rats assessed by contrast-enhanced and T2-weighted MRI.
Andreas Pohlmann, Lorna C Tilling, Alison Robinson, Olga Woolmer, Scott McCleary, Huw D Lewis

Inflamm Bowel Dis· April 2009

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The novel gamma secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) reduces amyloid plaque deposition without evidence of notch-related pathology in the Tg2576 mouse.
Jonathan D Best, David W Smith, Michael A Reilly, Ruth O'Donnell, Huw D Lewis

J Pharmacol Exp Ther· February 2007

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Apoptosis in T cell acute lymphoblastic leukemia cells after cell cycle arrest induced by pharmacological inhibition of notch signaling.
Huw D Lewis, Matthew Leveridge, Peter R Strack, Christine D Haldon, Jennifer O'neil

Chem Biol· February 2007

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A comparative assessment of gamma-secretase activity in transgenic and non-transgenic rodent brain.
Julian L Goggi, Huw D Lewis, Joanie Mok, Tim Harrison, Mark S Shearman

J Neurosci Methods· October 2006

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Intra- or intercomplex binding to the gamma-secretase enzyme. A model to differentiate inhibitor classes.
Earl E Clarke, Ian Churcher, Semantha Ellis, Jonathan D J Wrigley, Huw D Lewis

J Biol Chem· October 2006

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3-Substituted gem-cyclohexane sulfone based gamma-secretase inhibitors for Alzheimer's disease: conformational analysis and biological activity.
Richard A Jelley, Jason Elliott, Karl R Gibson, Timothy Harrison, Dirk Beher, Huw D Lewis

Bioorg Med Chem Lett· July 2006

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4-substituted cyclohexyl sulfones as potent, orally active gamma-secretase inhibitors.
Ian Churcher, Dirk Beher, Jonathan D Best, José L Castro, Earl E Clarke, Huw D Lewis

Bioorg Med Chem Lett· January 2006

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Quantitative measurement of changes in amyloid-beta(40) in the rat brain and cerebrospinal fluid following treatment with the gamma-secretase inhibitor LY-411575 [N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide].
Jonathan D Best, Mark T Jay, Franklin Otu, Jerome Ma, Alan Nadin, Huw D Lewis

J Pharmacol Exp Ther· May 2005

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Novel aspects of accumulation dynamics and A beta composition in transgenic models of AD.
Huw D Lewis, Dirk Beher, David Smith, Louise Hewson, Natalie Cookson

Neurobiol Aging· October 2004

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High affinity, bioavailable 3-amino-1,4-benzodiazepine-based gamma-secretase inhibitors.
Andrew P Owens, Alan Nadin, Adam C Talbot, Earl E Clarke, Timothy Harrison, Huw D Lewis

Bioorg Med Chem Lett· November 2003

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