Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Thomas Seal"'
Autor:
Antonia J. Lewis, Anna K. Bassil, Lee Andrew Harrison, Darren Jason Mitchell, Dave Lugo, Robert J. Watson, James Gray, Rab K. Prinjha, Alex Preston, Anne-Marie Michon, Ian D. Wall, Simon Taylor, Chun-wa Chung, Jonathan Thomas Seal, Stephen John Atkinson, Etienne Levernier, Paola Grandi, Emmanuel Hubert Demont, Inmaculada Rioja, James Michael Woolven, Cassie Messenger
Publikováno v:
Journal of Medicinal Chemistry. 64:10742-10771
Domain-specific BET bromodomain ligands represent an attractive target for drug discovery with the potential to unlock the therapeutic benefits of antagonizing these proteins without eliciting the toxicological aspects seen with pan-BET inhibitors. W
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d61563a5d35b9e5dc33735f58cc99285
https://doi.org/10.1021/acs.jmedchem.0c02155
https://doi.org/10.1021/acs.jmedchem.0c02155
Autor:
Emmanuel Hubert Demont, Jonathan Thomas Seal, Stephen John Atkinson, Anna K. Bassil, Paola Grandi, Robert J. Watson, Thomas George Christopher Hayhow, James Gray, Chun-wa Chung, Aylott Helen Elizabeth, Alexander N Phillipou, Darren Jason Mitchell, James Michael Woolven, Inmaculada Rioja, Laurie J. Gordon, Francesco Rianjongdee, Paul Bamborough, Ian D. Wall, Rab K. Prinjha, Alex Preston, Lee Andrew Harrison, Cassie Messenger
Publikováno v:
Journal of Medicinal Chemistry. 64:3249-3281
A number of reports have recently been published describing the discovery and optimization of bromo and extraterminal inhibitors which are selective for the second bromodomain (BD2); these include our own work toward GSK046 (3) and GSK620 (5). This p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::654a0dddd40ac85f0e3f79a9cc1d806c
https://doi.org/10.1021/acs.jmedchem.0c02156
https://doi.org/10.1021/acs.jmedchem.0c02156
Autor:
Stephen John Atkinson, Royston C. B. Copley, Matthew J Lindon, Rab K. Prinjha, Alex Preston, James Michael Woolven, Jonathan Thomas Seal, Chun-wa Chung, James Gray, Thomas George Christopher Hayhow, Laurie J. Gordon, Emmanuel Hubert Demont, Aylott Helen Elizabeth, Paola Grandi, Lee Andrew Harrison, Inmaculada Rioja, Robert J. Watson, Simon Taylor, Cassie Messenger, Ian D. Wall, Anne-Marie Michon, Darren Jason Mitchell, Paul Bamborough
Publikováno v:
'Journal of Medicinal Chemistry ', vol: 63, pages: 9093-9126 (2020)
The profound efficacy, yet associated toxicity of pan-BET inhibitors is well documented. The possibility of an ameliorated safety profile driven by significantly selective (>100-fold) inhibition of a subset of the eight bromodomains is enticing, but
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1ffc7e0a3296beacf38dc0ad074f7d92
https://doi.org/10.1021/acs.jmedchem.0c00796
https://doi.org/10.1021/acs.jmedchem.0c00796
Autor:
Peter D. Craggs, Darren Jason Mitchell, Rab K. Prinjha, Alex Preston, James Michael Woolven, Laurie J. Gordon, Simon Taylor, Paul Bamborough, Chun-wa Chung, Paola Grandi, James Gray, Francesco Rianjongdee, Matthew J Lindon, Anne-Marie Michon, Emma J. Jones, Inmaculada Rioja, Robert J. Watson, Ian D. Wall, Stephen John Atkinson, Emmanuel Hubert Demont, Jonathan Thomas Seal
Publikováno v:
Journal of Medicinal Chemistry. 63:9070-9092
Pan-bromodomain and extra terminal domain (BET) inhibitors interact equipotently with the eight bromodomains of the BET family of proteins and have shown profound efficacy in a number of in vitro phenotypic assays and in vivo pre-clinical models in i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::14bbc64ea8752fc9e9a4248fc67f1896
https://doi.org/10.1021/acs.jmedchem.0c00605
https://doi.org/10.1021/acs.jmedchem.0c00605
Autor:
Alex Phillipou, Ryan G. Kruger, Simon Taylor, Chun-wa Chung, Rab K. Prinjha, Laurie J. Gordon, Robert J. Watson, James Gray, Alex Preston, James J. Foley, Cassie Messenger, Anna K. Bassil, Inmaculada Rioja, James Michael Woolven, Xi-Ping Zhang, Francesco Rianjongdee, Paola Grandi, Jeanne J. Matteo, Anastasia Wyce, Ian D. Wall, Paul Bamborough, Darren Jason Mitchell, Lee Andrew Harrison, Michael T. McCabe, Stephen John Atkinson, Jonathan Thomas Seal, Emmanuel Hubert Demont
Publikováno v:
Journal of medicinal chemistry. 64(15)
The profound efficacy of pan-BET inhibitors is well documented, but these epigenetic agents have shown pharmacology-driven toxicity in oncology clinical trials. The opportunity to identify inhibitors with an improved safety profile by selective targe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a4e26e07fd3767cf6b96980599351c38
https://pubmed.ncbi.nlm.nih.gov/34255512
https://pubmed.ncbi.nlm.nih.gov/34255512
Autor:
Christopher Sedlacek, James Silvanima, Rick Copeland, Andy Woeber, Thomas Seal, Stephanie Sunderman-Barnes
Publikováno v:
Environmental monitoring and assessment. 190(7)
Current wastewater treatment technologies do not remove many unregulated hydrophilic compounds, and there is growing interest that low levels of these compounds, referred to as emerging contaminants, may impact human health and the environment. A pro
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::69740dffcf4b5b9fd9d4b223ef7d5a56
https://pubmed.ncbi.nlm.nih.gov/29951939
https://pubmed.ncbi.nlm.nih.gov/29951939
Autor:
Colin A. Campbell, Martin Rüdiger, Kevin Lee, Jason Witherington, Isobel Harada, Rab K. Prinjha, Umesh Kumar, Simon Taylor, Neil D. Christensen, Rebecca C. Furze, Ian D. Holyer, Mary A. Morse, Sarah A. Brendle, Mao X. Chen, Jonathan Thomas Seal, Karla K. Balogh
Publikováno v:
Antiviral research. 154
The DNA papillomaviruses infect squamous epithelium and can cause persistent, benign and sometimes malignant hyperproliferative lesions. Effective antiviral drugs to treat human papillomavirus (HPV) infection are lacking and here we investigate the a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::25d26616eb6352689d207bff033fbeef
https://pubmed.ncbi.nlm.nih.gov/29653131
https://pubmed.ncbi.nlm.nih.gov/29653131
Autor:
Jonathan Thomas Seal, Jonathan D. Goodacre, Chun-wa Chung, Laurie J. Gordon, Antonia J. Lewis, Paul Bamborough, David Matthew Wilson, Hawa Diallo, Woodrow Michael David
Publikováno v:
Journal of Medicinal Chemistry. 55:587-596
Bromodomains are epigenetic reader modules that regulate gene transcription through their recognition of acetyl-lysine modified histone tails. Inhibitors of this protein-protein interaction have the potential to modulate multiple diseases as demonstr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d07987ae62ceb0ce8778018753996e77
https://doi.org/10.1021/jm201283q
https://doi.org/10.1021/jm201283q
Autor:
Anne Marie Jeanne Bouillot, Frédéric Donche, Olivier Mirguet, Rab K. Prinjha, Gael Krysa, Edwige Nicodeme, Ann Louise Walker, Chun-wa Chung, Laurie J. Gordon, Kevin Lee, Soren Beinke, David Matthew Wilson, Inma Rioja, Toni Lewis, Leanne Cutler, Dave Lugo, Jonathan Thomas Seal, Jason Witherington, Paul Bamborough, Yann Lamotte, Scott McCleary, Jorge Kirilovsky, Françoise Gellibert
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(8)
A novel series of quinoline isoxazole BET family bromodomain inhibitors are discussed. Crystallography is used to illustrate binding modes and rationalize their SAR. One member, I-BET151 (GSK1210151A), shows good oral bioavailability in both the rat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::efda9004d594274ddcec17c62b1aae4d
https://pubmed.ncbi.nlm.nih.gov/22437115
https://pubmed.ncbi.nlm.nih.gov/22437115
Autor:
Delphine Delannée, Agnès Costaz, Jonathan Thomas Seal, Lionel Trottet, Rémi Tellier, Jean-Marie Brusq, Olivier Mirguet, Anne Marie Jeanne Bouillot, Sandrine Martin, Gael Krysa, Anne-Benedicte Boullay, Jorge Kirilovsky, Eric Boursier, Jérôme Toum, Yann Dudit, Van-Loc Nguyen, Edwige Nicodeme, Françoise Gellibert, Alizon M. Riou, Pascal Huet, Romain Luc Marie Gosmini, Yann Lamotte, Florence Blandel, Frédéric Donche
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(8)
The discovery, synthesis and biological evaluation of a novel series of 7-isoxazoloquinolines is described. Several analogs are shown to increase ApoA1 expression within the nanomolar range in the human hepatic cell line HepG2.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::30974817f673615f23351a44033e69cf
https://pubmed.ncbi.nlm.nih.gov/22386529
https://pubmed.ncbi.nlm.nih.gov/22386529