Targeting EZH2 as cancer therapy

DOI PDF PDF Web Site PubMed 1 Citations 32 References Open Access

Search this article

Description

<jats:title>Abstract</jats:title> <jats:p>Enhancer of zeste homolog 2 (EZH2) is the catalytic subunit of polycomb repressive complex 2 (PRC2) that mediate repression of target genes by trimethylation of Lys27 in histone 3 (H3K27me3). Given the reported roles of EZH2 in cancer, it is perhaps not surprising that targeting EZH2 in cancer therapy has become a hot research topic. Indeed, different types of EZH2 inhibitors are currently under development and are being evaluated by clinical trials. Recently, Murashima et al. identified NPD13668, a novel EZH2 inhibitor, by using a cell-based high-throughput screening assay. NPD13668 inhibited EZH2 methyltransferase activity, and repressed cell growth in multiple cancer cell lines, indicating a potential role for this compound in cancer treatment. In this review, we will focus on the current knowledge regarding the biological significance of PRC2 and H3K27me, and the recent advances in developing and testing drugs that target PRC2.</jats:p>

Journal

Citations (1)*help

See more

References(32)*help

See more

Related Projects

See more

Keywords

Details 詳細情報について

Report a problem

Back to top