CEINGE-Biotecnologie Avanzate, s.c.a r.l., Via G. Salvatore 486, 80145 Naples, Italy.
Biochem J. 2011 Aug 15;438(1):121-31. doi: 10.1042/BJ20101633.
AF4 belongs to a family of proteins implicated in childhood lymphoblastic leukaemia, FRAXE (Fragile X E site) mental retardation and ataxia. AF4 is a transcriptional activator that is involved in transcriptional elongation. Although AF4 has been implicated in MLL (mixed-lineage leukaemia)-related leukaemogenesis, AF4-dependent physiological mechanisms have not been clearly defined. Proteins that interact with AF4 may also play important roles in mediating oncogenesis, and are potential targets for novel therapies. Using a functional proteomic approach involving tandem MS and bioinformatics, we identified 51 AF4-interacting proteins of various Gene Ontology categories. Approximately 60% participate in transcription regulatory mechanisms, including the Mediator complex in eukaryotic cells. In the present paper we report one of the first extensive proteomic studies aimed at elucidating AF4 protein cross-talk. Moreover, we found that the AF4 residues Thr(220) and Ser(212) are phosphorylated, which suggests that AF4 function depends on phosphorylation mechanisms. We also mapped the AF4-interaction site with CDK9 (cyclin-dependent kinase 9), which is a direct interactor crucial for the function and regulation of the protein. The findings of the present study significantly expand the number of putative members of the multiprotein complex formed by AF4, which is instrumental in promoting the transcription/elongation of specific genes in human cells.
AF4 属于一种蛋白家族,该家族蛋白与儿童成淋巴细胞性白血病、脆性 X 智力迟钝和共济失调(FRAXE)有关。AF4 是一种转录激活因子,参与转录延伸。尽管 AF4 与混合谱系白血病(MLL)相关白血病的发生有关,但 AF4 依赖的生理机制尚未明确界定。与 AF4 相互作用的蛋白也可能在介导致癌作用中发挥重要作用,是新疗法的潜在靶点。我们使用涉及串联 MS 和生物信息学的功能蛋白质组学方法,鉴定了各种基因本体类别中的 51 种 AF4 相互作用蛋白。约 60%的蛋白参与转录调控机制,包括真核细胞中的中介复合物。在本论文中,我们报告了首次旨在阐明 AF4 蛋白串扰的广泛蛋白质组学研究之一。此外,我们发现 AF4 残基 Thr(220)和 Ser(212)发生磷酸化,这表明 AF4 功能取决于磷酸化机制。我们还绘制了与 CDK9(细胞周期蛋白依赖性激酶 9)的 AF4 相互作用位点,CDK9 是该蛋白功能和调节的关键直接相互作用因子。本研究的发现极大地扩展了由 AF4 形成的多蛋白复合物的假定成员数量,这对于促进人类细胞中特定基因的转录/延伸至关重要。