Department of Molecular and Cellular Oncology, The University of Texas M.D. Anderson Cancer Center, Houston, TX 77030, USA.
Nat Cell Biol. 2011 Jan;13(1):87-94. doi: 10.1038/ncb2139. Epub 2010 Dec 5.
Enhancer of zeste homologue 2 (EZH2) is the catalytic subunit of Polycomb repressive complex 2 (PRC2) and catalyses the trimethylation of histone H3 on Lys 27 (H3K27), which represses gene transcription. EZH2 enhances cancer-cell invasiveness and regulates stem cell differentiation. Here, we demonstrate that EZH2 can be phosphorylated at Thr 487 through activation of cyclin-dependent kinase 1 (CDK1). The phosphorylation of EZH2 at Thr 487 disrupted EZH2 binding with the other PRC2 components SUZ12 and EED, and thereby inhibited EZH2 methyltransferase activity, resulting in inhibition of cancer-cell invasion. In human mesenchymal stem cells, activation of CDK1 promoted mesenchymal stem cell differentiation into osteoblasts through phosphorylation of EZH2 at Thr 487. These findings define a signalling link between CDK1 and EZH2 that may have an important role in diverse biological processes, including cancer-cell invasion and osteogenic differentiation of mesenchymal stem cells.
增强子结合锌指蛋白 2(EZH2)是多梳抑制复合物 2(PRC2)的催化亚基,催化组蛋白 H3 赖氨酸 27(H3K27)的三甲基化,从而抑制基因转录。EZH2 增强癌细胞的侵袭性并调节干细胞分化。在这里,我们证明 cyclin-dependent kinase 1(CDK1)的激活可以使 EZH2 在 Thr 487 位磷酸化。EZH2 在 Thr 487 位的磷酸化破坏了 EZH2 与其他 PRC2 成分 SUZ12 和 EED 的结合,从而抑制了 EZH2 甲基转移酶活性,导致癌细胞侵袭的抑制。在人类间充质干细胞中,CDK1 的激活通过 EZH2 在 Thr 487 位的磷酸化促进间充质干细胞向成骨细胞分化。这些发现定义了 CDK1 和 EZH2 之间的信号联系,它可能在包括癌细胞侵袭和间充质干细胞成骨分化在内的多种生物学过程中发挥重要作用。