ORY-1001, a Potent and Selective Covalent KDM1A Inhibitor, for the Treatment of Acute Leukemia

The lysine-specific demethylase KDM1A is a key regulator of stem cell potential in acute myeloid leukemia (AML). ORY-1001 is a highly potent and selective KDM1A inhibitor that induces H3K4me2 accumulation on KDM1A target genes, blast differentiation, and reduction of leukemic stem cell capacity in A...

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Veröffentlicht in:	Cancer cell 2018-03, Vol.33 (3), p.495-511.e12
Hauptverfasser:	Maes, Tamara, Mascaró, Cristina, Tirapu, Iñigo, Estiarte, Angels, Ciceri, Filippo, Lunardi, Serena, Guibourt, Nathalie, Perdones, Alvaro, Lufino, Michele M.P., Somervaille, Tim C.P., Wiseman, Dan H., Duy, Cihangir, Melnick, Ari, Willekens, Christophe, Ortega, Alberto, Martinell, Marc, Valls, Nuria, Kurz, Guido, Fyfe, Matthew, Castro-Palomino, Julio Cesar, Buesa, Carlos
Format:	Artikel
Sprache:	eng
Schlagworte:	acute myeloid leukemia Animals Apoptosis - drug effects Cell Differentiation - drug effects Cell Line, Tumor - metabolism differentiation Disease Models, Animal epigenetic Histone Demethylases - antagonists & inhibitors Histone Demethylases - drug effects Histone Demethylases - genetics histone methylation Humans KDM1A Leukemia, Myeloid, Acute - drug therapy Leukemia, Myeloid, Acute - genetics LSD1 Mice ORY-1001 Stem Cells - drug effects Stem Cells - metabolism
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