Cheng Y C
Biochim Biophys Acta. 1976 Dec 8;452(2):370-81. doi: 10.1016/0005-2744(76)90186-8.
Deoxythymidine kinases (EC 2.7.1.--) induced in HeLa TK- cells by Herpes simplex Type I and Type II viruses both had a requirement for divalent cations. The enzymes had the highest activities in the presence of Mg2+, followed by Mn2+, Ca2+, Fe2+, and in that order, whereas they were inactive in the presence of Zn2+ and Cu2+. The amount of Mg2+ required for optimal activity was dependent on the amount of ATP present, so that optimal activities were found when the concentration of Mg2+ was equal to that of ATP; an excess of Mg2+ inhibited the reaction. The activities of various nucleoside triphosphates as phosphate donors for Herpes simplex virus Type I deoxythymidine kinase were in the order: ATP = dATP = ara ATP greater than CTP greater than dCTP greater than UTP greater than dUTP greater than GTP greater than dGTP. Those for Herpes simplex virus Type II deoxythymidine kinase were in the order: CTP greater than dCTP = ara CTP greater than dATP greater than ATP greater than UTP greater than GTP greater than dUTP = dGTP. For both deoxythymidine kinases induced by Herpes simplex virus, the nucleoside triphosphates tested exerted cooperative effects. The Km values of ATP and CTP for the Herpes simplex virus Type I enzyme were 30 and 70 muM respectively; whereas those for the Herpes simplex virus Typr II enzyme were 140 and 450 muM. Studies on binding of various thymidine analogs with free 5'-OH to these deoxythymidine kinases indicated that 5-substituted ethyl-, vinyl-, allyl-, propyl-, iodo- and bromo-dUrd as well as iodo5 dCyd and bromo5 dCyd had good affinity to both enzymes. In contrast, vinyl5 Urd, iodo5 Urd and arabinosylthymidine had good affinity only to the Herpes simplex virus Type I enzyme but not to the Herpes simplex virus Type II deoxythymidine kinase. All of these thymidine analogs were competitive inhibitors, with KI values in the range of 0.25 to 1.5 muM. Herpes simplex virus Type I deoxythymidine kinase was less sensitive to either dTTP or iodo dUTP inhibition than Herpes simplex virus Type II. Both dThd and dCyd could serve as substrates and competed with each other for Herpes simplex viruses Type I and Type II induced kinases, but they differed in their Km values for these enzymes. The Km values of dThd and dCyd were 0.59 muM and 25 muM for Herpes simplex virus Type I deoxythymidine kinase; while they were 0.36 muM and 88 muM respectively for the Herpes simplex virus Type II enzyme.
I型和II型单纯疱疹病毒在HeLa TK-细胞中诱导产生的脱氧胸苷激酶(EC 2.7.1.--)都需要二价阳离子。这些酶在Mg2+存在时活性最高,其次是Mn2+、Ca2+、Fe2+,且顺序依次如此,而在Zn2+和Cu2+存在时则无活性。最佳活性所需的Mg2+量取决于ATP的存在量,因此当Mg2+浓度等于ATP浓度时可发现最佳活性;Mg2+过量会抑制反应。作为I型单纯疱疹病毒脱氧胸苷激酶磷酸供体的各种核苷三磷酸的活性顺序为:ATP = dATP = ara ATP>CTP>dCTP>UTP>dUTP>GTP>dGTP。II型单纯疱疹病毒脱氧胸苷激酶的活性顺序为:CTP>dCTP = ara CTP>dATP>ATP>UTP>GTP>dUTP = dGTP。对于由单纯疱疹病毒诱导产生的两种脱氧胸苷激酶,所测试的核苷三磷酸都发挥协同作用。I型单纯疱疹病毒酶对ATP和CTP的Km值分别为30和70μM;而II型单纯疱疹病毒酶的Km值分别为140和450μM。对各种带有游离5'-OH的胸苷类似物与这些脱氧胸苷激酶结合的研究表明,5-取代的乙基、乙烯基、烯丙基、丙基、碘代和溴代脱氧尿苷以及碘代5-脱氧胞苷和溴代5-脱氧胞苷对这两种酶都有良好的亲和力。相比之下,乙烯基5-尿苷、碘代5-尿苷和阿糖胸苷仅对I型单纯疱疹病毒酶有良好的亲和力,而对II型单纯疱疹病毒脱氧胸苷激酶没有亲和力。所有这些胸苷类似物都是竞争性抑制剂,KI值在0.25至1.5μM范围内。I型单纯疱疹病毒脱氧胸苷激酶对dTTP或碘代dUTP抑制的敏感性低于II型单纯疱疹病毒。dThd和dCyd都可作为底物,并相互竞争I型和II型单纯疱疹病毒诱导的激酶,但它们对这些酶的Km值不同。I型单纯疱疹病毒脱氧胸苷激酶对dThd和dCyd的Km值分别为0.59μM和25μM;而II型单纯疱疹病毒酶的Km值分别为0.36μM和88μM。