Ontology highlight
ABSTRACT:
SUBMITTER: Horton JR
PROVIDER: S-EPMC4958579 | biostudies-literature | 2016 Jul
REPOSITORIES: biostudies-literature
Cell chemical biology 20160714 7
The KDM5/JARID1 family of Fe(II)- and α-ketoglutarate-dependent demethylases removes methyl groups from methylated lysine 4 of histone H3. Accumulating evidence supports a role for KDM5 family members as oncogenic drivers. We compare the in vitro inhibitory properties and binding affinity of ten diverse compounds with all four family members, and present the crystal structures of the KDM5A-linked Jumonji domain in complex with eight of these inhibitors in the presence of Mn(II). All eight inhibi ...[more]