A Novel Cell-Permeable, Selective, and Noncompetitive Inhibitor of KAT3 Histone Acetyltransferases from a Combined Molecular Pruning/Classical Isosterism Approach

Selective inhibitors of the two paralogue KAT3 acetyltransferases (CBP and p300) may serve not only as precious chemical tools to investigate the role of these enzymes in physiopathological mechanisms but also as lead structures for the development of further antitumor agents. After the application...

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Veröffentlicht in:	Journal of medicinal chemistry 2015-03, Vol.58 (6), p.2779-2798
Hauptverfasser:	Milite, Ciro, Feoli, Alessandra, Sasaki, Kazuki, La Pietra, Valeria, Balzano, Amodio Luca, Marinelli, Luciana, Mai, Antonello, Novellino, Ettore, Castellano, Sabrina, Tosco, Alessandra, Sbardella, Gianluca
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetylation - drug effects Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Cell Cycle Checkpoints - drug effects Cell Line, Tumor Cell Survival - drug effects Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Histones - metabolism Humans Leukemia - drug therapy Leukemia - enzymology Leukemia - metabolism Lysine - metabolism Models, Molecular p300-CBP Transcription Factors - antagonists & inhibitors p300-CBP Transcription Factors - metabolism
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