PT - JOURNAL ARTICLE AU - HIROTSUGU SAKAKI AU - MASASHI OKADA AU - KENTA KURAMOTO AU - HIROYUKI TAKEDA AU - HIKARU WATARAI AU - SHUHEI SUZUKI AU - SHIZUKA SEINO AU - MANABU SEINO AU - TSUYOSHI OHTA AU - SATORU NAGASE AU - HIROHISA KURACHI AU - CHIFUMI KITANAKA TI - GSKJ4, A Selective Jumonji H3K27 Demethylase Inhibitor, Effectively Targets Ovarian Cancer Stem Cells DP - 2015 Dec 01 TA - Anticancer Research PG - 6607--6614 VI - 35 IP - 12 4099 - http://ar.iiarjournals.org/content/35/12/6607.short 4100 - http://ar.iiarjournals.org/content/35/12/6607.full SO - Anticancer Res2015 Dec 01; 35 AB - Background/Aim: Global increase in the trimethylation of histone H3 at lysine 27 (H3K27me3) has been associated with the differentiation of normal stem cells and cancer cells, however, the role of H3K27me3 in the control of cancer stem cells (CSCs) remains poorly understood. We investigated the impact of increased H3K27me3 on CSCs using a selective H3K27 demethylase inhibitor GSKJ4. Materials and Methods: The effect of GSKJ4 on the viability as well as on the self-renewal and tumor-initiating capacity of CSCs derived from the A2780 human ovarian cancer cell line was examined. Results: GSKJ4 induced cell death in A2780 CSCs at a concentration non-toxic to normal human fibroblasts. GSKJ4 also caused loss of self-renewal and tumor-initiating capacity of A2780 CSCs surviving GSKJ4 treatment. Conclusion: Our findings suggest that H3K27 methylation may have an inhibitory role in the maintenance of CSCs and that GSKJ4 may represent a novel class of CSC-targeting agents.