Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Cassie Messenger"'
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
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:
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:
H. Christian Eberl, Ken G. M. Fantom, Francesca Zappacosta, David J. Fallon, Jacob T. Bush, Emma K. Grant, Nicholas C. O. Tomkinson, Cassie Messenger
Publikováno v:
Angewandte Chemie International Edition. 58:17322-17327
The CDK family plays a crucial role in the control of the cell cycle. Dysregulation and mutation of the CDKs has been implicated in cancer and the CDKs have been investigated extensively as potential therapeutic targets. Selective inhibition of speci
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:
Lee A, Harrison, Stephen J, Atkinson, Anna, Bassil, Chun-Wa, Chung, Paola, Grandi, James R J, Gray, Etienne, Levernier, Antonia, Lewis, David, Lugo, Cassie, Messenger, Anne-Marie, Michon, Darren J, Mitchell, Alex, Preston, Rab K, Prinjha, Inmaculada, Rioja, Jonathan T, Seal, Simon, Taylor, Ian D, Wall, Robert J, Watson, James M, Woolven, Emmanuel H, Demont
Publikováno v:
Journal of medicinal chemistry. 64(15)
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:
Peter D. Craggs, Faith Mazani, Gabriella Clarke, Carl Haslam, Bhumika Karamshi, Paul Rowland, Sam Rowe, Luke A Greenhough, Ryan P. Bingham, Cassie Messenger, Alexander N Phillipou
Publikováno v:
SLAS discovery : advancing life sciences RD. 26(5)
The predominant assay detection methodologies used for enzyme inhibitor identification during early-stage drug discovery are fluorescence-based. Each fluorophore has a characteristic fluorescence decay, known as the fluorescence lifetime, that occurs
Autor:
Emma J. Jones, Charles S. Lay, Charlotte E. Carver, John P. Evans, Kristopher McCombe, Alexander N Phillipou, Daniel Thomas, Peter D. Craggs, Cassie Messenger, Mahnoor Mahmood, Kelly M Gatfield, Kristin M. Riching, Laurie J. Gordon, Matthew Campbell
Publikováno v:
Cell chemical biology. 29(2)
Contemporary drug discovery typically quantifies the effect of a molecule on a biological target using the equilibrium-derived measurements of IC50, EC50, or KD. Kinetic descriptors of drug binding are frequently linked with the effectiveness of a mo