Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Antonia J. Lewis"'
Autor:
Han Dai, Robert P. Law, John P. Evans, Gillian F. Watt, Chun-wa Chung, Markus A. Queisser, John D. Harling, Antonia J. Lewis, Marcus Bantscheff, João Osvaldo Rodrigues Nunes, Adam Flinders, Paul Scott-Stevens, Andrew B. Benowitz, Peter Stacey, Christopher J. Tame, Karol Buda, Diana Klimaszewska, Marcel Muelbaier, Nico Zinn
Publikováno v:
Angewandte Chemie. 133:23515-23522
Focal adhesion kinase (FAK) is a key mediator of tumour progression and metastasis. To date, clinical trials of FAK inhibitors have reported disappointing efficacy for oncology indications. We report the design and characterisation of GSK215, a poten
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::78bf53bda7c0c58ce1f7c8658407374a
https://doi.org/10.1002/ange.202109237
https://doi.org/10.1002/ange.202109237
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:
Anne-Marie Michon, Rab K. Prinjha, Alex Preston, Laurie J. Gordon, Inmaculada Rioja, Pierre Thesmar, Emmanuel Hubert Demont, James Michael Woolven, Stephen John Atkinson, Jon T. Seal, Cassie Messenger, Lee Andrew Harrison, Paola Grandi, Darren Jason Mitchell, Robert J. Watson, Simon Taylor, Chun-wa Chung, James Gray, Antonia J. Lewis, Ian D. Wall, Dave Lugo, Paul Bamborough
Publikováno v:
ACS Med Chem Lett
[Image: see text] Pan-BET inhibitors have shown profound efficacy in a number of in vivo preclinical models and have entered the clinic in oncology trials where adverse events have been reported. These inhibitors interact equipotently with the eight
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a25fcee7700cf48b3d9393a0adacecd2
https://doi.org/10.1021/acsmedchemlett.0c00247
https://doi.org/10.1021/acsmedchemlett.0c00247
Autor:
Patricia F Medeiros, Mythily Vimal, Vipulkumar Kantibhai Patel, John Evans, Neil R Carlson, Antonia J. Lewis, Paul Bamborough, Katherine L Jones, Jane E Smith, Michael O'Sullivan, Scott McCleary, Darren J. Mitchell, Heather Barnett, Chun-wa Chung, Gang Yao, Anthony W. J. Cooper, Rab K. Prinjha, Laurie Gordon, Mahnoor Mahmood, Peter D. Craggs, Isobel L Harada, Rino A Bit, Natalie Wellaway, Armelle Le Gall, Robert J. Watson, Tony W Dean, Dominique Amans, Ian D. Wall, Kayleigh A J Stafford, Dave Lugo, Matthew J Lindon, Rishi R Shah, David Jonathan Hirst, Chris Patten, Darren L Poole, Jack A Brown, Philip G Humphreys, Robert P Davis, Christopher Roland Wellaway, Pamela J Thomas
Publikováno v:
Journal of Medicinal Chemistry. 63:714-746
The bromodomain and extraterminal (BET) family of bromodomain-containing proteins are important regulators of the epigenome through their ability to recognize N-acetyl lysine (KAc) post-translational modifications on histone tails. These interactions
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fdb502737af78aed357d47636c87313d
https://doi.org/10.1021/acs.jmedchem.9b01670
https://doi.org/10.1021/acs.jmedchem.9b01670
Autor:
James M. Woolven, William J. Kerr, Chun-wa Chung, Bhumika Karamshi, Beata S. Wyspiańska, John Evans, Emmanuel Hubert Demont, Laurie Gordon, Matthew J Lindon, Peter E. Soden, Rob Willis, Leanne Cutler, Darren J. Mitchell, Christopher Roland Wellaway, Antonia J. Lewis, Robert J. Watson, Paul Bamborough, Simon Taylor, Inmaculada Rioja, Sharon G. Bernard, Rab K. Prinjha, Peter D. Craggs
The bromodomain and extraterminal domain (BET) family of epigenetic regulators comprises four proteins (BRD2, BRD3, BRD4, BRDT), each containing tandem bromodomains. To date, small molecule inhibitors of these proteins typically bind all eight bromod
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a2071ff9f599969eeda5e1e32f456446
https://strathprints.strath.ac.uk/73542/1/Wellaway_etal_JMC_2020_Structure_based_design_of_a_bromodomain_and_extraterminal_domain_BET_inhibitor.pdf
https://strathprints.strath.ac.uk/73542/1/Wellaway_etal_JMC_2020_Structure_based_design_of_a_bromodomain_and_extraterminal_domain_BET_inhibitor.pdf
Autor:
Cassie Messenger, Laurie J. Gordon, Simon C. C. Lucas, Aaron T. Cheng, Kelly M Gatfield, John P. Evans, Emma J. Jones, Mahnoor Mahmood, Charles S. Lay, Charlotte E. Carver, Douglas Sammon, Antonia J. Lewis, Alexander N Phillipou, Syandan Chakraborty, Luke A Greenhough, Peter D. Craggs, David J Brierley
Publikováno v:
SLAS discovery : advancing life sciences RD. 25(2)
Malfunctions in the basic epigenetic mechanisms such as histone modifications, DNA methylation, and chromatin remodeling are implicated in a number of cancers and immunological and neurodegenerative conditions. Within GlaxoSmithKline (GSK) we have ut
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bc63556b946b71c8a1576c30413bb503
https://pubmed.ncbi.nlm.nih.gov/31875412
https://pubmed.ncbi.nlm.nih.gov/31875412
Autor:
Chun-wa Chung, Rab K. Prinjha, Rejbinder Kaur, Peter Ernest Soden, Ann Louise Walker, Van Loc Nguyen, Christophe Simon, Simon Taylor, Romain Luc Marie Gosmini, Jean-Marie Brusq, Antonia J. Lewis, Mark B. Schilling, Lionel Trottet, Matthew D. Walker, Leanne Cutler, Olivier Mirguet, Emmanuel Hubert Demont, Edwige Nicodeme, Eric Boursier, Jérôme Toum, Alizon M. Riou-Eymard, Gael Krysa, Hugh Clark, Paul Bamborough
Publikováno v:
Journal of Medicinal Chemistry. 57:8111-8131
Through their function as epigenetic readers of the histone code, the BET family of bromodomain-containing proteins regulate expression of multiple genes of therapeutic relevance, including those involved in tumor cell growth and inflammation. BET br
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0406fa8ebf77977076028bacf4d90daa
https://doi.org/10.1021/jm5010539
https://doi.org/10.1021/jm5010539
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:
Chun-wa Chung, Mélanie Barnathan, Phillip Jeffrey, Nicholas Smithers, Romain Luc Marie Gosmini, Olivier Pineau, Jacqueline Elizabeth Mordaunt, Jason Witherington, Alain Claude-Marie Daugan, Myriam Ajakane, Leanne Cutler, Paul Bamborough, Nigel J. Parr, Jean-Marie Brusq, Iain Uings, Andrea C. Haynes, Antonia J. Lewis, Jérôme Toum, Rab K. Prinjha, Olivier Mirguet, Catherine A. Clément, Edwige Nicodeme, Miriam Crowe, Grimes Richard Martin
Publikováno v:
Journal of medicinal chemistry. 56(19)
The bromo and extra C-terminal domain (BET) family of bromodomains are involved in binding epigenetic marks on histone proteins, more specifically acetylated lysine residues. This paper describes the discovery and structure–activity relationships (
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8b0781caa707d63e5ebf47768737d8a9
https://pubmed.ncbi.nlm.nih.gov/24107192
https://pubmed.ncbi.nlm.nih.gov/24107192
Autor:
Delphine Delannée, Pascal Huet, Chun-wa Chung, Anne Marie Jeanne Bouillot, Françoise Gellibert, Antonia J. Lewis, Yann Lamotte, Yann Dudit, Lionel Trottet, Jason Witherington, Olivier Mirguet, Edwige Nicodeme, Paul Bamborough, Gael Krysa
Publikováno v:
ChemMedChem. 9(3)
Bromodomains (BRDs) are small protein domains found in a variety of proteins that recognize and bind to acetylated histone tails. This binding affects chromatin structure and facilitates the localisation of transcriptional complexes to specific genes
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e3113f2253c473e9878b834d1652ca2a
https://pubmed.ncbi.nlm.nih.gov/24000170
https://pubmed.ncbi.nlm.nih.gov/24000170