Major Michael L, Lepe Rita, Costa Robert H
Department of Biochemistry and Molecular Genetics, College of Medicine, University of Illinois at Chicago, Chicago, Illinois 60607, USA.
Mol Cell Biol. 2004 Apr;24(7):2649-61. doi: 10.1128/MCB.24.7.2649-2661.2004.
Previous liver regeneration studies demonstrated that the mouse forkhead box M1B (FoxM1B) transcription factor regulates hepatocyte proliferation through expression of cell cycle genes that stimulate cyclin-dependent kinase 2 (Cdk2) and Cdk1 activity. In this study, we demonstrated that disruption of the FoxM1B Cdk1/2 phosphorylation site at Thr residue 596 significantly reduced both FoxM1B transcriptional activity and Cdk phosphorylation of the FoxM1B T596A mutant protein in vivo. Retention of this FoxM1B 596 Cdk phosphorylation site was found to be essential for recruiting the histone acetyltransferase CREB binding protein (CBP) to the FoxM1B transcriptional activation domain. Consistent with these findings, dominant negative Cdk1 protein significantly reduced FoxM1B transcriptional activity and inhibited FoxM1B recruitment of the CBP coactivator protein. Likewise, Cdc25B-mediated stimulation of Cdk activity together with elevated levels of the CBP coactivator protein provided a 6.2-fold synergistic increase in FoxM1B transcriptional activity. Furthermore, mutation of the FoxM1B Leu 641 residue within an LXL motif (residues 639 to 641) inhibited recruitment of Cdk-cyclin complexes and caused significant reduction in both FoxM1B transcriptional activity and in vivo Cdk phosphorylation of the FoxM1B Thr 596 residue. We demonstrated that FoxM1B transcriptional activity requires binding of either S-phase or M-phase Cdk-cyclin complexes to mediate efficient Cdk phosphorylation of the FoxM1B Thr 596 residue, which is essential for recruitment of p300/CBP coactivator proteins.
以往的肝脏再生研究表明,小鼠叉头框M1B(FoxM1B)转录因子通过刺激细胞周期蛋白依赖性激酶2(Cdk2)和Cdk1活性的细胞周期基因的表达来调节肝细胞增殖。在本研究中,我们证明,在体内,FoxM1B第596位苏氨酸(Thr)残基处的Cdk1/2磷酸化位点的破坏显著降低了FoxM1B转录活性以及FoxM1B T596A突变蛋白的Cdk磷酸化。发现保留该FoxM1B 596 Cdk磷酸化位点对于将组蛋白乙酰转移酶CREB结合蛋白(CBP)募集到FoxM1B转录激活域至关重要。与这些发现一致,显性负性Cdk1蛋白显著降低了FoxM1B转录活性,并抑制了CBP共激活蛋白的FoxM1B募集。同样,Cdc25B介导的Cdk活性刺激以及CBP共激活蛋白水平的升高使FoxM1B转录活性协同增加了6.2倍。此外,LXL基序(第639至641位残基)内的FoxM1B第641位亮氨酸(Leu)残基的突变抑制了Cdk-细胞周期蛋白复合物的募集,并导致FoxM1B转录活性以及FoxM1B第596位苏氨酸残基的体内Cdk磷酸化显著降低。我们证明,FoxM1B转录活性需要S期或M期Cdk-细胞周期蛋白复合物的结合来介导FoxM1B第596位苏氨酸残基的有效Cdk磷酸化,这对于募集p300/CBP共激活蛋白至关重要。