Naphthyridines as Novel BET Family Bromodomain Inhibitors

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, thereby regulating epigenetically controlled pro...

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Veröffentlicht in:	ChemMedChem 2014-03, Vol.9 (3), p.580-589
Hauptverfasser:	Mirguet, Olivier, Lamotte, Yann, Chung, Chun-wa, Bamborough, Paul, Delannée, Delphine, Bouillot, Anne, Gellibert, Françoise, Krysa, Gael, Lewis, Antonia, Witherington, Jason, Huet, Pascal, Dudit, Yann, Trottet, Lionel, Nicodeme, Edwige
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Anti-Inflammatory Agents, Non-Steroidal - chemistry Anti-Inflammatory Agents, Non-Steroidal - pharmacology BET family bromodomains inhibitors Chromatin Chromosomal Proteins, Non-Histone Crystallography, X-Ray Dose-Response Relationship, Drug epigenetic readers Histones - chemistry Histones - metabolism inflammation Mice Mice, Inbred BALB C Models, Molecular Molecular Structure naphthyridines Naphthyridines - chemistry Naphthyridines - pharmacology Nuclear Proteins - antagonists & inhibitors Nuclear Proteins - metabolism Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Protein Structure, Tertiary - drug effects Protein-Serine-Threonine Kinases - antagonists & inhibitors Protein-Serine-Threonine Kinases - metabolism Structure-Activity Relationship Transcription Factors - antagonists & inhibitors Transcription Factors - metabolism
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