Tetrazolylhydrazides as Selective Fragment-Like Inhibitors of the JumonjiC-Domain-Containing Histone Demethylase KDM4A

The JumonjiC‐domain‐containing histone demethylase 2A (JMJD2A, KDM4A) is a key player in the epigenetic regulation of gene expression. Previous publications have shown that both elevated and lowered enzyme levels are associated with certain types of cancer, and therefore the definite role of KDM4A i...

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Veröffentlicht in:	ChemMedChem 2015-11, Vol.10 (11), p.1875-1883
Hauptverfasser:	Rüger, Nicole, Roatsch, Martin, Emmrich, Thomas, Franz, Henriette, Schüle, Roland, Jung, Manfred, Link, Andreas
Format:	Artikel
Sprache:	eng
Schlagworte:	acyl hydrazides acyl hydrazones Dose-Response Relationship, Drug Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology epigenetics histone demethylase Humans Hydrazines - chemical synthesis Hydrazines - chemistry Hydrazines - pharmacology Jumonji Domain-Containing Histone Demethylases - antagonists & inhibitors Jumonji Domain-Containing Histone Demethylases - metabolism Molecular Structure Structure-Activity Relationship tetrazoles Tetrazoles - chemical synthesis Tetrazoles - chemistry Tetrazoles - pharmacology
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