Casimiro Mathew C, Wang Chenguang, Li Zhiping, Di Sante Gabriele, Willmart Nicole E, Addya Sankar, Chen Lei, Liu Yang, Lisanti Michael P, Pestell Richard G
Department of Cancer Biology, Kimmel Cancer Center, Thomas Jefferson University, Philadelphia, Pennsylvania 19107, USA.
Mol Endocrinol. 2013 Sep;27(9):1415-28. doi: 10.1210/me.2013-1065. Epub 2013 Jul 17.
The CCND1 gene, which is frequently overexpressed in cancers, encodes the regulatory subunit of a holoenzyme that phosphorylates the retinoblastoma protein. Although it is known that cyclin D1 regulates estrogen receptor (ER)α transactivation using heterologous reporter systems, the in vivo biological significance of cyclin D1 to estrogen-dependent signaling, and the molecular mechanisms by which cyclin D1 is involved, are yet to be elucidated. Herein, genome-wide expression profiling conducted of 17β-estradiol-treated castrated virgin mice deleted of the Ccnd1 gene demonstrated that cyclin D1 determines estrogen-dependent gene expression for 88% of estrogen-responsive genes in vivo. In addition, expression profiling of 17β-estradiol-stimulated cyclin D1 small interfering RNA treated MCF7 cells shows cyclin D1 is required for estrogen-mediated gene expression in vitro. Genome-wide chromatin immunoprecipitation-Seq analysis revealed a cyclin D1-DNA bound form associated with genes that were regulated by estrogen in a cyclin D1-dependent manner. The cyclin D1-dependent estrogen signaling pathways identified in vivo were highly enriched for extracellular membrane-associated growth factor receptors (epidermal growth factor receptor, ErbB3, and EphB3) and their ligands (amphiregulin, encoded by AREG gene), and matrix metalloproteinase. The AREG protein, a pivotal ligand for epidermal growth factor receptors to promote cellular proliferation, was induced by cyclin D1 via the AREG promoter. Chromatin immunoprecipitation analysis demonstrated the recruitment of cyclin D1 to the breast cancer 1 (Brca1)/ERα binding site of the Areg gene. Cyclin D1 genetic deletion demonstrated the in vivo requirement for cyclin D1 in assembling the estrogen-dependent amplified in breast cancer 1-associated multiprotein complex. The current studies define a requirement for cyclin D1 in estrogen-dependent signaling modules governing growth factor receptor and ligand expression in vivo and reveal a noncanonical function of cyclin D1 at ERα target gene promoters. Cyclin D1 mediates the convergence of ERα and growth factor signaling at a common cis-element of growth factor genes.
CCND1基因在癌症中经常过度表达,它编码一种全酶的调节亚基,该全酶可使视网膜母细胞瘤蛋白磷酸化。虽然已知细胞周期蛋白D1使用异源报告系统调节雌激素受体(ER)α的反式激活,但细胞周期蛋白D1对雌激素依赖性信号传导的体内生物学意义以及其涉及的分子机制仍有待阐明。在此,对缺失Ccnd1基因的17β-雌二醇处理的去势处女小鼠进行全基因组表达谱分析,结果表明细胞周期蛋白D1在体内决定了88%的雌激素反应基因的雌激素依赖性基因表达。此外,对17β-雌二醇刺激的细胞周期蛋白D1小干扰RNA处理的MCF7细胞进行表达谱分析表明,细胞周期蛋白D1是体外雌激素介导的基因表达所必需的。全基因组染色质免疫沉淀测序分析揭示了一种细胞周期蛋白D1-DNA结合形式,其与以细胞周期蛋白D1依赖性方式受雌激素调节的基因相关。在体内鉴定出的细胞周期蛋白D1依赖性雌激素信号通路高度富集细胞外膜相关生长因子受体(表皮生长因子受体、ErbB3和EphB3)及其配体(由AREG基因编码的双调蛋白)和基质金属蛋白酶。双调蛋白(AREG)是表皮生长因子受体促进细胞增殖的关键配体,它由细胞周期蛋白D1通过AREG启动子诱导产生。染色质免疫沉淀分析表明细胞周期蛋白D1被募集到Areg基因的乳腺癌1(Brca1)/ERα结合位点。细胞周期蛋白D1基因缺失表明在体内组装雌激素依赖性乳腺癌1相关多蛋白复合物时需要细胞周期蛋白D1。当前研究确定了细胞周期蛋白D1在体内雌激素依赖性信号模块中对生长因子受体和配体表达的需求,并揭示了细胞周期蛋白D1在ERα靶基因启动子处的非经典功能。细胞周期蛋白D1在生长因子基因的共同顺式元件处介导ERα和生长因子信号的汇聚。