Výsledky vyhledávání - "Huw D. Lewis"

Akademický článek

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

Autor: Andrew Y. F. Li Yim, Enrico Ferrero, Klio Maratou, Huw D. Lewis, George Royal, David F. Tough, Chris Larminie, Marcel M. A. M. Mannens, Peter Henneman, Wouter J. de Jonge, Marleen G. H. van de Sande, Danielle M. Gerlag, Rab K. Prinjha, Paul P. Tak

Publikováno v: Frontiers in Immunology, Vol 12 (2021)

In this study, we sought to characterize synovial tissue obtained from individuals with arthralgia and disease-specific auto-antibodies and patients with established rheumatoid arthritis (RA), by applying an integrative multi-omics approach where we

Externí odkaz: https://doaj.org/article/b65fadd8bd9d4285968860c81c44f2e9

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Phase 1 and preclinical profiling of ESM‐HDAC391, a myeloid‐targeted histone deacetylase inhibitor, shows enhanced pharmacology and monocytopaenia

Autor: Rebecca C. Furze, Judit Molnar, Nigel J. Parr, Faiz Ahmad, Yvette Henry, David Howe, Rajendra Singh, Martin Toal, Anna K. Bassil, Sharon G. Bernard, Robert P. Davis, Adele Gibson, N. Claire Maller, Catriona Sharp, David F. Tough, Rab K. Prinjha, Huw D. Lewis

Publikováno v: British Journal of Clinical Pharmacology. 88:5238-5256

To improve the tolerability and therapeutic application of histone deacetylase inhibitors (HDACi), by application of an esterase-sensitive motif (ESM), to target pharmacological activity directly to mononuclear myeloid cells expressing the processing

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b986a405b103538adcd6ab638dd0581c
https://doi.org/10.1111/bcp.15428

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Akademický článek

Targeting Histone Deacetylases in Myeloid Cells Inhibits Their Maturation and Inflammatory Function With Limited Effects on Atherosclerosis

Autor: Rosario Luque-Martin, Jan Van den Bossche, Rebecca C. Furze, Annette E. Neele, Saskia van der Velden, Marion J.J. Gijbels, Cindy P.P.A. van Roomen, Sharon G. Bernard, Wouter J. de Jonge, Inmaculada Rioja, Rab K. Prinjha, Huw D. Lewis, Palwinder K. Mander, Menno P.J. de Winther

Publikováno v: Frontiers in Pharmacology, Vol 10 (2019)

Monocytes and macrophages are key drivers in the pathogenesis of inflammatory diseases. Epigenetic targets have been shown to control the transcriptional profile and phenotype of these cells. Since histone deacetylase protein inhibitors demonstrate p

Externí odkaz: https://doaj.org/article/0bd1c20ec87342d695539812e636ba12

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Carboxylesterase-1 Assisted Targeting of HDAC Inhibitors to Mononuclear Myeloid Cells in Inflammatory Bowel Disease

Publikováno v: Elfiky, A M I, Ghiboub, M, Li Yim, A Y F, Hageman, I L, Verhoeff, J, de Krijger, M, van Hamersveld, P H P, Welting, O, Admiraal, I, Rahman, S, Garcia-Vallejo, J J, Wildenberg, M E, Tomlinson, L, Gregory, R, Rioja, I, Prinjha, R K, Furze, R C, Lewis, H D, Mander, P K, Heinsbroek, S E M, Bell, M J & de Jonge, W J 2022, ' Carboxylesterase-1 Assisted Targeting of HDAC Inhibitors to Mononuclear Myeloid Cells in Inflammatory Bowel Disease ', Journal of Crohn's and Colitis, vol. 16, no. 4, pp. 668-681 . https://doi.org/10.1093/ecco-jcc/jjab176
Journal of Crohn's and Colitis, 16(4), 668-681. Elsevier
Journal of Crohn's & colitis, 16(4), 668-681. Elsevier

Background and AimsHistone deacetylase inhibitors [HDACi] exert potent anti-inflammatory effects. Because of the ubiquitous expression of HDACs, clinical utility of HDACi is limited by off-target effects. Esterase-sensitive motif [ESM] technology aim

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::082c0316620861e7964614f67286a50a
https://doi.org/10.1093/ecco-jcc/jjab176

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Preclinical models of arthritis for studying immunotherapy and immune tolerance

Autor: Pascale Wehr, Daniela Sieghart, Shaima Al Khabouri, György Nagy, Michael Bonelli, Gavin R. Meehan, Catharien M. U. Hilkens, James M. Brewer, Ranjeny Thomas, Paul Garside, Huw D. Lewis, David C. Wraith, David F. Tough

Publikováno v: Annals of the Rheumatic Diseases

Increasingly earlier identification of individuals at high risk of rheumatoid arthritis (RA) (eg, with autoantibodies and mild symptoms) improves the feasibility of preventing or curing disease. The use of antigen-specific immunotherapies to reinstat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bffd263ffa34d2645071950755643de5
https://doi.org/10.1136/annrheumdis-2021-220043

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Discovery of potent and selective Spleen Tyrosine Kinase inhibitors for the topical treatment of inflammatory skin disease

Autor: Michael David Barker, Emma J. Jones, Robert J. Watson, Huw D. Lewis, Cesar Ramirez-Molina, David Matthew Wilson, Marion C. Dickson, Robert P. Davis, Francis Louis Atkinson, Margarete Neu, Donald O. Somers, John Liddle

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 28:3458-3462

The discovery and lead optimisation of a novel series of SYK inhibitors is described. These were optimised for SYK potency and selectivity against Aurora B. Compounds were profiled in a human skin penetration study to identify a suitable candidate mo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ea0edda7c25304f4d66d8a85ae30e56a
https://doi.org/10.1016/j.bmcl.2018.09.022

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Optimisation of a novel series of potent and orally bioavailable azanaphthyridine SYK inhibitors

Autor: Alex Preston, Scott McCleary, Emma J. Jones, Huw D. Lewis, Michael David Barker, Robert J. Watson, Tracy Jane Shipley, Cesar Ramirez-Molina, Dave Lugo, Clement Douault, Robert P. Davis, David Matthew Wilson, Margarete Neu, Neil Stuart Garton, Edward Hooper-Greenhill, John Liddle, Don O. Somers

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 26:4606-4612

The optimisation of the azanaphthyridine series of Spleen Tyrosine Kinase inhibitors is described. The medicinal chemistry strategy was focused on optimising the human whole blood activity whilst achieving a sufficient margin over hERG activity. A go

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::60c70f363fa050d5a84cc13aacffd65e
https://doi.org/10.1016/j.bmcl.2016.08.070

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