JmjC ‐domain‐Containing Histone Demethylases

The Clinically Used Iron Chelator Deferasirox Is an Inhibitor of Epigenetic JumonjiC Domain-Containing Histone Demethylases

“…JmjC histone demethylases have emerged as promising drug targets, ,− with inhibitor discovery programs being reported by us − and others, − as recently reviewed. ,,− A majority of reported JmjC KDM inhibitors function by active site metal chelation and competitive displacement of the co-substrate 2OG. − Very recently, covalent KDM5 inhibitors , and inhibitors of both the lysyl- and arginyl-demethylase activities have also been reported.…”

Oxygen-dependent histone lysine demethylase 4 restricts hepatitis B virus replication

“…S1 A ). Phylogenetic analysis identified homology between KDM4 and 5 ( 35 ), and we expanded our analysis to include KDM4 ( 36 ). We observed a striking increase in the levels of pC/pgRNA and total HBV RNAs after inhibiting KDM4 with QC6352, accompanied by an increase in the levels of H3K9 trimethylation and limited evidence of cytotoxicity ( Figs.…”

Oxygen-Dependent Histone Lysine Demethylase 4 Restricts Hepatitis B Virus Replication

“…S1A). Phylogenetic analysis identified homology between KDM4 and 5 (35), and we expanded our analysis to include KDM4 (36). We observed a striking increase in the levels of pC/pgRNA and total HBV RNAs after inhibiting KDM4 with QC6352, accompanied by an increase in the levels of H3K9 trimethylation and limited evidence of cytotoxicity (Figs.…”