Zobrazeno 1 - 10
of 64
pro vyhledávání: '"Emmanuel Hubert Demont"'
Autor:
Stephen John Atkinson, Patricia F Medeiros, Paola Grandi, Simon Taylor, Chun-wa Chung, James Gray, Robert J. Watson, Ian D. Wall, Alexander L. Satz, Rab K. Prinjha, Francesco Rianjongdee, Alex Preston, Emmanuel Hubert Demont, Gang Yao, Alex Phillipou, Inmaculada Rioja, Cassie Messenger, Laura J. Kaushansky
Publikováno v:
Journal of Medicinal Chemistry. 64:10806-10833
Second-generation bromodomain and extra terminal (BET) inhibitors, which selectively target one of the two bromodomains in the BET proteins, have begun to emerge in the literature. These inhibitors aim to help determine the roles and functions of eac
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a6ff4ecfe9cbf342e44c1ed73c09a9fc
https://doi.org/10.1021/acs.jmedchem.1c00412
https://doi.org/10.1021/acs.jmedchem.1c00412
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:
Peter Ernest Soden, Massimo Petretich, Robert J. Watson, Laurie J. Gordon, Chun-wa Chung, Paola Grandi, Alex Phillipou, Paul Bamborough, Emmanuel Hubert Demont, Rab K. Prinjha, Inmaculada Rioja, Thilo Werner, Robert E. Davis, Heather A. Barnett
Publikováno v:
Journal of Medicinal Chemistry. 63:9045-9069
Pan-bromodomain and extra terminal (BET) inhibitors interact equipotently with all eight bromodomains of the BET family of proteins. They have shown profound efficacy in vitro and in vivo in oncology and immunomodulatory models, and a number of them
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c3697424bf0dce94f0fb982a9f330e0e
https://doi.org/10.1021/acs.jmedchem.0c00614
https://doi.org/10.1021/acs.jmedchem.0c00614
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:
Ian D. Wall, Thomas Grimes, Laurie J. Gordon, James Michael Woolven, Simon Taylor, Robert P. Davis, Simon C. C. Lucas, Chun-wa Chung, James J R Gray, Paola Grandi, Nicholas C. O. Tomkinson, Rab K. Prinjha, Robert J. Watson, Inmaculada Rioja, Alex Preston, Alexander N Phillipou, Stephen John Atkinson, Emmanuel Hubert Demont
Herein, a series of 2,3-dihydrobenzofurans have been developed as highly potent bromo and extra-terminal domain (BET) inhibitors with 1000-fold selectivity for the second bromodomain (BD2) over the first bromodomain (BD1). Investment in the developme
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::547bee46f66a5c9178b4a1bb02762f95
https://strathprints.strath.ac.uk/78085/1/Lucas_etal_JMC_2021_Optimization_of_a_series_of_2_3_dihydrobenzofurans_as_highly_potent_second_bromodomain.pdf
https://strathprints.strath.ac.uk/78085/1/Lucas_etal_JMC_2021_Optimization_of_a_series_of_2_3_dihydrobenzofurans_as_highly_potent_second_bromodomain.pdf
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:
Emmanuel Hubert Demont, Philip G. Humphreys, Alex Phillipou, Michael A. Clegg, Paul Bamborough, Peter D. Craggs, Chun-wa Chung, Rab K. Prinjha, Gemma Michele Liwicki, Nicholas C. O. Tomkinson, Natalie Hope Theodoulou, Laurie J. Gordon
Publikováno v:
ACS Med Chem Lett
[Image: see text] Bromodomain containing proteins and the acetyl-lysine binding bromodomains contained therein are increasingly attractive targets for the development of novel epigenetic therapeutics. To help validate this target class and unravel th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a371aaebd689aa1b81c6ef189c8b2232
https://pubmed.ncbi.nlm.nih.gov/34413961
https://pubmed.ncbi.nlm.nih.gov/34413961