Department of Medical Microbiology, Immunology and Cell Biology, Southern Illinois University School of Medicine, Springfield, IL 62794, U.S.A.
Biochem J. 2010 Oct 15;431(2):227-35. doi: 10.1042/BJ20100558.
A sole EBV (Epstein-Barr virus)-encoded protein kinase (EBV-PK) (the BGLF4 gene product) plays important roles in viral infection. Although a number of targets of this protein have been identified, the kinase itself remains largely unstudied with regard to its enzymology and structure. In the present study, site-directed mutagenesis has been employed to generate mutations targeting residues involved in nuclear localization of the EBV-PK, core residues in subdomain III of the protein kinase domain conserved in most protein kinases or residues in subdomain VIa conserved only within the HPK (herpesvirus-encoded protein kinase) group. Deletion of amino acids 389-391 resulted in exclusive cytoplasmic localization of the protein, indicating the involvement of this region in nuclear translocation of the EBV-PK. Mutations at the amino acids Glu113 (core component), Phe175, Leu178, Phe184, Leu185 and Asn186 (conserved in HPKs) resulted in loss of EBV-PK autophosphorylation, protein substrate [EBV EA-D (early antigen diffused)] phosphorylation, and ability to facilitate ganciclovir phosphorylation. These results reiterate the unique features of this group of kinases and present an opportunity for designing more specific antiviral compounds.
一种单纯疱疹病毒(EBV)编码的蛋白激酶(EBV-PK)(BGLF4 基因产物)在病毒感染中发挥重要作用。尽管已经鉴定出这种蛋白的许多靶标,但对于其酶学和结构,激酶本身在很大程度上仍未得到研究。在本研究中,采用定点突变技术生成了针对 EBV-PK 核定位、蛋白激酶结构域中 III 亚结构域核心残基(大多数蛋白激酶中保守)或仅在 HPK(疱疹病毒编码的蛋白激酶)组中保守的 VIa 亚结构域残基的突变。氨基酸 389-391 的缺失导致蛋白仅定位于细胞质,表明该区域参与 EBV-PK 的核易位。氨基酸 Glu113(核心成分)、Phe175、Leu178、Phe184、Leu185 和 Asn186(HPKs 中保守)的突变导致 EBV-PK 自身磷酸化、蛋白底物 [EBV EA-D(早期抗原弥散)] 磷酸化和促进更昔洛韦磷酸化的能力丧失。这些结果重申了这组激酶的独特特征,并为设计更具特异性的抗病毒化合物提供了机会。