A specific JMJD6 inhibitor potently suppresses multiple types of cancers both in vitro and in vivo.

ABSTRACT: Jumonji C-domain-containing protein 6 (JMJD6), an iron (Fe²⁺) and α-ketoglutarate (α-KG)-dependent oxygenase, is expressed at high levels, correlated with poor prognosis, and considered as a therapeutic target in multiple cancer types. However, specific JMJD6 inhibitors that are potent in suppressing tumorigenesis have not been reported so far. We herein report that iJMJD6, a specific small-molecule inhibitor of JMJD6 with favorable physiochemical properties, inhibits the enzymatic activity of JMJD6 protein both in vitro and in cultured cells. iJMJD6 is effective in suppressing cell proliferation, migration, and invasion in multiple types of cancer cells in a JMJD6-dependent manner, while it exhibits minimal toxicity in normal cells. Mechanistically, iJMJD6 represses the express

SUBMITTER: Xiao RQ 

PROVIDER: S-EPMC9407455 | biostudies-literature | 2022 Aug

REPOSITORIES: biostudies-literature