Varambally Sooryanarayana, Dhanasekaran Saravana M, Zhou Ming, Barrette Terrence R, Kumar-Sinha Chandan, Sanda Martin G, Ghosh Debashis, Pienta Kenneth J, Sewalt Richard G A B, Otte Arie P, Rubin Mark A, Chinnaiyan Arul M
Department of Pathology, University of Michigan Medical School, Ann Arbor, Michigan 48109, USA.
Nature. 2002 Oct 10;419(6907):624-9. doi: 10.1038/nature01075.
Prostate cancer is a leading cause of cancer-related death in males and is second only to lung cancer. Although effective surgical and radiation treatments exist for clinically localized prostate cancer, metastatic prostate cancer remains essentially incurable. Here we show, through gene expression profiling, that the polycomb group protein enhancer of zeste homolog 2 (EZH2) is overexpressed in hormone-refractory, metastatic prostate cancer. Small interfering RNA (siRNA) duplexes targeted against EZH2 reduce the amounts of EZH2 protein present in prostate cells and also inhibit cell proliferation in vitro. Ectopic expression of EZH2 in prostate cells induces transcriptional repression of a specific cohort of genes. Gene silencing mediated by EZH2 requires the SET domain and is attenuated by inhibiting histone deacetylase activity. Amounts of both EZH2 messenger RNA and EZH2 protein are increased in metastatic prostate cancer; in addition, clinically localized prostate cancers that express higher concentrations of EZH2 show a poorer prognosis. Thus, dysregulated expression of EZH2 may be involved in the progression of prostate cancer, as well as being a marker that distinguishes indolent prostate cancer from those at risk of lethal progression.
前列腺癌是男性癌症相关死亡的主要原因,仅次于肺癌。尽管对于临床局限性前列腺癌存在有效的手术和放射治疗方法,但转移性前列腺癌基本上仍无法治愈。在此我们通过基因表达谱分析表明,多梳蛋白家族成员zeste同源物2(EZH2)在激素难治性转移性前列腺癌中过度表达。针对EZH2的小干扰RNA(siRNA)双链体可减少前列腺细胞中EZH2蛋白的量,并在体外抑制细胞增殖。EZH2在前列腺细胞中的异位表达诱导特定一组基因的转录抑制。由EZH2介导的基因沉默需要SET结构域,并通过抑制组蛋白脱乙酰酶活性而减弱。转移性前列腺癌中EZH2信使RNA和EZH2蛋白的量均增加;此外,表达较高浓度EZH2的临床局限性前列腺癌预后较差。因此,EZH2表达失调可能参与前列腺癌的进展,并且是区分惰性前列腺癌与有致命进展风险的前列腺癌的标志物。