The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor

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 challenging given the close homology. Herein, w...

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Veröffentlicht in:	Journal of medicinal chemistry 2020-09, Vol.63 (17), p.9093-9126
Hauptverfasser:	Seal, Jonathan T, Atkinson, Stephen J, Aylott, Helen, Bamborough, Paul, Chung, Chun-wa, Copley, Royston C. B, Gordon, Laurie, Grandi, Paola, Gray, James R. J, Harrison, Lee A, Hayhow, Thomas G, Lindon, Matthew, Messenger, Cassie, Michon, Anne-Marie, Mitchell, Darren, Preston, Alex, Prinjha, Rab K, Rioja, Inmaculada, Taylor, Simon, Wall, Ian D, Watson, Robert J, Woolven, James M, Demont, Emmanuel H
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Amides - chemistry Amides - metabolism Amides - pharmacokinetics Animals Anti-Inflammatory Agents - chemistry Anti-Inflammatory Agents - metabolism Anti-Inflammatory Agents - pharmacokinetics Binding Sites Cell Cycle Proteins - antagonists & inhibitors Cell Cycle Proteins - metabolism Crystallography, X-Ray Dogs Half-Life Humans Hydrogen Bonding Ligands Male Molecular Dynamics Simulation Protein Domains Rats Rats, Wistar Structure-Activity Relationship Transcription Factors - antagonists & inhibitors Transcription Factors - metabolism
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