Département de Biologie, Faculté des Sciences, Université de Sherbrooke, Sherbrooke, Quebec, Canada.
EMBO J. 2011 Aug 12;30(19):3947-61. doi: 10.1038/emboj.2011.284.
Chromatin represents a repressive barrier to the process of ligand-dependent transcriptional activity of nuclear receptors. Here, we show that H3K27 methylation imposes ligand-dependent regulation of the oestrogen receptor α (ERα)-dependent apoptotic response via Bcl-2 in breast cancer cells. The activation of BCL2 transcription is dependent on the simultaneous inactivation of the H3K27 methyltransferase, EZH2, and the demethylation of H3K27 at a poised enhancer by the ERα-dependent recruitment of JMJD3 in hormone-dependent breast cancer cells. We also provide evidence that this pathway is modified in cells resistant to anti-oestrogen (AE), which constitutively express BCL2. We show that the lack of H3K27 methylation at BCL2 regulatory elements due to the inactivation of EZH2 by the HER2 pathway leads to this constitutive activation of BCL2 in these AE-resistant cells. Our results describe a mechanism in which the epigenetic state of chromatin affects ligand dependency during ERα-regulated gene expression.
染色质代表核受体配体依赖性转录活性过程中的一种抑制性障碍。在这里,我们表明 H3K27 甲基化通过乳腺癌细胞中的 Bcl-2 对雌激素受体 α (ERα) 依赖性凋亡反应施加配体依赖性调节。BCL2 转录的激活依赖于同时失活 H3K27 甲基转移酶 EZH2,以及在激素依赖性乳腺癌细胞中通过 ERα 依赖性募集 JMJD3 使 H3K27 在准备好的增强子上发生去甲基化。我们还提供了证据表明,该途径在对抗雌激素(AE)有抗性的细胞中发生了改变,这些细胞持续表达 BCL2。我们表明,由于 HER2 途径使 EZH2 失活,BCL2 调控元件处缺乏 H3K27 甲基化导致这些 AE 抗性细胞中 BCL2 的持续激活。我们的结果描述了一种机制,其中染色质的表观遗传状态影响 ERα 调节基因表达过程中的配体依赖性。