Bruck Nathalie, Vitoux Dominique, Ferry Christine, Duong Vanessa, Bauer Annie, de Thé Hughes, Rochette-Egly Cécile
Department of Functional Genomics, Institut de Génétique et de Biologie Moléculaire et Cellulaire, INSERM U596, CNRS UMR7104, Université Louis Pasteur de Strasbourg, CU de Strasbourg, France.
EMBO J. 2009 Jan 7;28(1):34-47. doi: 10.1038/emboj.2008.256. Epub 2008 Dec 11.
The nuclear retinoic acid (RA) receptor alpha (RARalpha) is a transcriptional transregulator that controls the expression of specific gene subsets through binding at response elements and dynamic interactions with coregulators, which are coordinated by the ligand. Here, we highlighted a novel paradigm in which the transcription of RARalpha target genes is controlled by phosphorylation cascades initiated by the rapid RA activation of the p38MAPK/MSK1 pathway. We demonstrate that MSK1 phosphorylates RARalpha at S369 located in the ligand-binding domain, allowing the binding of TFIIH and thereby phosphorylation of the N-terminal domain at S77 by cdk7/cyclin H. MSK1 also phosphorylates histone H3 at S10. Finally, the phosphorylation cascade initiated by MSK1 controls the recruitment of RARalpha/TFIIH complexes to response elements and subsequently RARalpha target gene activation. Cancer cells characterized by a deregulated p38MAPK/MSK1 pathway, do not respond to RA, outlining the essential contribution of the RA-triggered phosphorylation cascade in RA signalling.
核视黄酸(RA)受体α(RARα)是一种转录反式调节因子,它通过与反应元件结合以及与共调节因子的动态相互作用来控制特定基因子集的表达,这些相互作用由配体协调。在此,我们突出了一种新的模式,即RARα靶基因的转录由p38丝裂原活化蛋白激酶/丝裂原和应激激活蛋白激酶1(p38MAPK/MSK1)途径的快速RA激活引发的磷酸化级联反应所控制。我们证明,MSK1在位于配体结合域的S369位点使RARα磷酸化,从而允许TFIIH的结合,进而使N端结构域在S77位点被周期蛋白依赖性激酶7/细胞周期蛋白H(cdk7/cyclin H)磷酸化。MSK1还在S10位点使组蛋白H3磷酸化。最后,由MSK1引发的磷酸化级联反应控制RARα/TFIIH复合物募集到反应元件,随后激活RARα靶基因。以p38MAPK/MSK1途径失调为特征的癌细胞对RA无反应,这突显了RA触发的磷酸化级联反应在RA信号传导中的重要作用。