Gartel A L, Ye X, Goufman E, Shianov P, Hay N, Najmabadi F, Tyner A L
Department of Molecular Genetics, University of Illinois College of Medicine, Chicago, IL 60607, USA.
Proc Natl Acad Sci U S A. 2001 Apr 10;98(8):4510-5. doi: 10.1073/pnas.081074898. Epub 2001 Mar 27.
The cyclin-dependent kinase inhibitor p21((WAF1/CIP1)) inhibits proliferation both in vitro and in vivo, and overexpression of p21 in normal and tumor cell lines results in cell cycle arrest. In contrast, ectopic expression of Myc alleviates G(1) cell cycle arrest. Recent studies showed that Myc can repress p21 transcription, thereby overriding a p21-mediated cell cycle checkpoint. We found that activation of a Myc-estrogen receptor fusion protein by 4-hydroxytamoxifen in mouse cells resulted in suppression of endogenous p21 transcription. This effect was observed in the absence of de novo protein synthesis and was independent of histone deacetylase activity. In transient transfection studies, Myc effectively repressed p21 promoter constructs containing only 119 bp of sequence upstream of the transcription start site. This region contains multiple Sp1-binding sites and a potential initiator element, but no canonical Myc DNA-binding sites. Deletion of the potential initiator element does not affect repression of the p21 promoter by c-Myc. Coimmunoprecipitation and glutathione S-transferase pull-down experiments demonstrate that c-Myc may form complexes with Sp1/Sp3. We found that the central region of c-Myc interacts with the zinc finger domain of Sp1. Because Sp1 is required for p21 transcription, it is possible that Myc may down-regulate p21 transcription, at least in part, by sequestering Sp1. Repression of the p21 promoter may contribute to the ability of c-Myc to promote cell proliferation.
细胞周期蛋白依赖性激酶抑制剂p21((WAF1/CIP1))在体外和体内均能抑制细胞增殖,在正常细胞系和肿瘤细胞系中过表达p21会导致细胞周期停滞。相反,Myc的异位表达可缓解G(1)期细胞周期停滞。最近的研究表明,Myc可抑制p21转录,从而越过p21介导的细胞周期检查点。我们发现,在小鼠细胞中用4-羟基他莫昔芬激活Myc-雌激素受体融合蛋白会导致内源性p21转录受到抑制。在没有从头合成蛋白质的情况下观察到了这种效应,并且该效应与组蛋白脱乙酰酶活性无关。在瞬时转染研究中,Myc有效地抑制了仅包含转录起始位点上游119 bp序列的p21启动子构建体。该区域包含多个Sp1结合位点和一个潜在的起始元件,但没有典型的Myc DNA结合位点。删除潜在的起始元件并不影响c-Myc对p21启动子的抑制作用。免疫共沉淀和谷胱甘肽S-转移酶下拉实验表明,c-Myc可能与Sp1/Sp3形成复合物。我们发现c-Myc的中央区域与Sp1的锌指结构域相互作用。由于Sp1是p21转录所必需的,因此Myc可能至少部分地通过隔离Sp1来下调p21转录。p21启动子的抑制可能有助于c-Myc促进细胞增殖的能力。