Introduction: As epigenetic modulators, histone demethylases can be a therapeutic target in the area of oncology. KDM4 subfamily proteins are histone demethylases with a Jumonji domain. The subfamily consists of five functional members: KDM4A, KDM4B, KDM4C, KDM4D, and KDM4E. The role of the KDM4 subfamily proteins is reported in oncogenesis, and their overexpression in various tumor types is observed. Small molecule inhibitors for KDM4 proteins have great potential in anti-cancer therapy.
Areas covered: A comprehensive review of the patents for KDM4 inhibitors is provided in this paper. Small molecule structural information and pharmacological effects are presented in the content.
Expert opinion: The status of KDM4 inhibitor development is still in the early stages with small numbers of patents and journal articles. Future KDM4 inhibitor development should focus on obtaining selectivity between KDM4 subtypes, development of small molecules with in vivo activity, and extension of the therapeutic area of KDM4 inhibitors other than use in cancer therapy.
Keywords: JHDM3; Jumonji D2; KDM4; epigenetics; histone demethylase.