Department of Parasitology, College of Medicine, National Taiwan University, Taipei 100, Taiwan, Republic of China.
J Biol Chem. 2012 Feb 3;287(6):3733-50. doi: 10.1074/jbc.M111.298893. Epub 2011 Dec 13.
The protozoan Giardia lamblia parasitizes the human small intestine to cause diseases. It undergoes differentiation into infectious cysts by responding to intestinal stimulation. How the activated signal transduction pathways relate to encystation stimulation remain largely unknown. During encystation, genes encoding cyst wall proteins (CWPs) are coordinately up-regulated by a Myb2 transcription factor. Because cell differentiation is linked to cell cycle regulation, we tried to understand the role of cell cycle regulators, cyclin-dependent kinases (Cdks), in encystation. We found that the recombinant Myb2 was phosphorylated by Cdk-associated complexes and the levels of phosphorylation increased significantly during encystation. We have identified a putative cdk gene (cdk2) by searching the Giardia genome database. Cdk2 was found to localize in the cytoplasm with higher expression during encystation. Interestingly, overexpression of Cdk2 resulted in a significant increase of the levels of cwp gene expression and cyst formation. In addition, the Cdk2-associated complexes can phosphorylate Myb2 and the levels of phosphorylation increased significantly during encystation. Mutations of important catalytic residues of Cdk2 resulted in a significant decrease of kinase activity and ability of inducing cyst formation. Addition of a Cdk inhibitor, purvalanol A, significantly decreased the Cdk2 kinase activity and the levels of cwp gene expression and cyst formation. Our results suggest that the Cdk2 pathway may be involved in phosphorylation of Myb2, leading to activation of the Myb2 function and up-regulation of cwp genes during encystation. The results provide insights into the use of Cdk inhibitory drugs in disruption of Giardia differentiation into cysts.
原虫蓝氏贾第鞭毛虫寄生在人类小肠中引起疾病。它通过对肠道刺激的反应分化为感染性囊。激活的信号转导途径如何与囊形成刺激相关在很大程度上仍然未知。在囊形成过程中,编码囊壁蛋白(CWP)的基因通过 Myb2 转录因子协同上调。由于细胞分化与细胞周期调控有关,我们试图了解细胞周期调节剂、细胞周期蛋白依赖性激酶(Cdk)在囊形成中的作用。我们发现重组 Myb2 被 Cdk 相关复合物磷酸化,并且在囊形成过程中磷酸化水平显著增加。我们通过搜索贾第虫基因组数据库鉴定了一个推定的 cdk 基因(cdk2)。发现 Cdk2 定位于细胞质中,在囊形成过程中表达水平较高。有趣的是,过表达 Cdk2 导致 cwp 基因表达和囊形成水平显著增加。此外,Cdk2 相关复合物可以磷酸化 Myb2,并且在囊形成过程中磷酸化水平显著增加。Cdk2 的重要催化残基突变导致激酶活性和诱导囊形成的能力显著降低。添加 Cdk 抑制剂 purvalanol A 显著降低了 Cdk2 激酶活性以及 cwp 基因表达和囊形成水平。我们的结果表明,Cdk2 途径可能参与 Myb2 的磷酸化,从而在囊形成过程中激活 Myb2 功能并上调 cwp 基因的表达。这些结果为利用 Cdk 抑制性药物破坏贾第虫分化为囊提供了新的见解。