Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Darren Jason Mitchell"'
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
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
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
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
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
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
Autor:
Chun-wa Chung, Rab K. Prinjha, Simon C. C. Lucas, Nicholas C. O. Tomkinson, Alexander N Phillipou, Stephen John Atkinson, Darren Jason Mitchell, Paul Bamborough, Robert J. Sheppard, Emmanuel Hubert Demont, Robert J. Watson, Laurie J. Gordon, Heather A. Barnett
Most bromodomain inhibitors mimic the interactions of the natural acetylated lysine (KAc) histone substrate through key interactions with conserved asparagine and tyrosine residues within the binding pocket. Herein we report the optimization of a ser
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b5846b0ef827565f0ccfd4008efb5659
https://strathprints.strath.ac.uk/73265/1/Lucas_etal_JMC_2020_The_optimisation_of_potent_ATAD2_and_CECR2_Bromodomain_inhibitors_with_an_atypical_binding_mode.pdf
https://strathprints.strath.ac.uk/73265/1/Lucas_etal_JMC_2020_The_optimisation_of_potent_ATAD2_and_CECR2_Bromodomain_inhibitors_with_an_atypical_binding_mode.pdf
Autor:
Andrew D. Roberts, Peter Francis, Paola Grandi, Emma J. Jones, David P. Dixon, Robert J. Watson, Christina Rau, Peter Pogány, Angela Bridges, Chun-wa Chung, Darren Jason Mitchell, Rab K. Prinjha, Peter D. Craggs, Kelly Locke, Emmanuel Hubert Demont, Anne-Marie Michon, Bhumika Karamshi, Rebecca C. Furze, Paul Bamborough, Robert J. Sheppard, Simon C. C. Lucas, Ana Maria Roa
Publikováno v:
Journal of medicinal chemistry. 62(16)
The bromodomain of ATAD2 has proved to be one of the least-tractable proteins within this target class. Here, we describe the discovery of a new class of inhibitors by high-throughput screening and show how the difficulties encountered in establishin
Autor:
Clement Douault, Tony Kouzarides, Robert J. Sheppard, Hawa Diallo, Paola Grandi, Samuel Robson, Chun-wa Chung, Ka Hing Che, Rab K. Prinjha, Richard J. Upton, Darren Jason Mitchell, Rebecca C. Furze, Emmanuel Hubert Demont, Andrew J. Bannister, Anne-Marie Michon, Robert J. Watson, Christina Rau, Paul Bamborough
Publikováno v:
Angew Chem Int Ed Engl
ATAD2 is a cancer-associated protein whose bromodomain has been described as among the least druggable of that target class. Starting from a potent lead, permeability and selectivity were improved through a dual approach: 1) using CF(2) as a sulfone
Autor:
Laurie J. Gordon, David J. Fallon, Heather A. Barnett, Chun-wa Chung, Darren Jason Mitchell, Emma J. Jones, Robert J. Watson, Rab K. Prinjha, Armelle Le Gall, Isabelle Becher, Paola Grandi, Emmanuel Hubert Demont, Edward Hooper-Greenhill, Peter D. Craggs, Mark J. Bird, Allan J. B. Watson, Hawa Diallo, Robert P. Law, Robert J. Sheppard, Anne-Marie Michon, Dave Lugo, Paul Bamborough, Clare I. Hobbs
Publikováno v:
ACS Medicinal Chemistry Letters. 7:552-557
The BRPF (Bromodomain and PHD Finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. A selective benzimidazolone BRPF1 inhibitor showing micromolar activity in a cellular target