Snowden A W, Anderson L A, Webster G A, Perkins N D
Division of Gene Regulation and Expression, Department of Biochemistry, University of Dundee, Dundee DD1 5EH, Scotland, United Kingdom.
Mol Cell Biol. 2000 Apr;20(8):2676-86. doi: 10.1128/MCB.20.8.2676-2686.2000.
The transcriptional coactivators p300 and CREB binding protein (CBP) are important regulators of the cell cycle, differentiation, and tumorigenesis. Both p300 and CBP are targeted by viral oncoproteins, are mutated in certain forms of cancer, are phosphorylated in a cell cycle-dependent manner, interact with transcription factors such as p53 and E2F, and can be found complexed with cyclinE-Cdk2 in vivo. Moreover, p300-deficient cells show defects in proliferation. Here we demonstrate that transcriptional activation by both p300 and CBP is stimulated by coexpression of the cyclin-dependent kinase inhibitor p21(WAF/CIP1). Significantly this stimulation is independent of both the inherent histone acetyltransferase (HAT) activity of p300 and CBP and of the previously reported carboxyl-terminal binding site for cyclinE-Cdk2. Rather, we describe a previously uncharacterized transcriptional repression domain (CRD1) within p300. p300 transactivation is stimulated through derepression of CRD1 by p21. Significantly p21 regulation of CRD1 is dependent on the nature of the core promoter. We suggest that CRD1 provides a novel mechanism through which p300 and CBP can switch activities between the promoters of genes that stimulate growth and those that enhance cell cycle arrest.
转录共激活因子p300和CREB结合蛋白(CBP)是细胞周期、分化和肿瘤发生的重要调节因子。p300和CBP均为病毒癌蛋白的作用靶点,在某些癌症中发生突变,以细胞周期依赖性方式被磷酸化,与p53和E2F等转录因子相互作用,并且在体内可与细胞周期蛋白E-Cdk2形成复合物。此外,p300缺陷型细胞在增殖方面表现出缺陷。在此我们证明,细胞周期蛋白依赖性激酶抑制剂p21(WAF/CIP1)的共表达可刺激p300和CBP的转录激活。重要的是,这种刺激既不依赖于p300和CBP固有的组蛋白乙酰转移酶(HAT)活性,也不依赖于先前报道的细胞周期蛋白E-Cdk2的羧基末端结合位点。相反,我们在p300中发现了一个以前未被描述的转录抑制结构域(CRD1)。p300的反式激活是通过p21对CRD1的去抑制作用来刺激的。重要的是,p21对CRD1的调节取决于核心启动子的性质。我们认为,CRD1提供了一种新机制,通过该机制p300和CBP可以在刺激生长的基因启动子和增强细胞周期停滞的基因启动子之间切换活性。