人类疱疹病毒 6 U69 激酶将甲基环丙烯核苷类化合物环丙氟达拉滨、MBX2168 和 MBX1616 磷酸化为单磷酸。
Human herpesvirus 6 U69 kinase phosphorylates the methylenecyclopropane nucleosides cyclopropavir, MBX 2168, and MBX 1616 to their monophosphates.
机构信息
Microbiotix, Inc., Worcester, Massachusetts, USA.
出版信息
Antimicrob Agents Chemother. 2013 Nov;57(11):5760-2. doi: 10.1128/AAC.00978-13. Epub 2013 Aug 26.
Abstract
Dihydroxymethyl and monohydroxymethyl methylenecyclopropane nucleosides are effective inhibitors of both variants of human herpesvirus 6 (HHV-6). We investigated involvement of HHV-6 U69 protein kinase in their mechanism of action. Phosphorylation of the dihydroxymethyl analogue cyclopropavir and monohydroxymethyl nucleosides with either a 6-ether moiety (MBX 2168) or a 6-thioether moiety (MBX 1616) with purified U69 was examined. All three compounds were substrates of this viral kinase and had similar Michaelis-Menten kinetic parameters.
摘要
二羟甲基和单羟甲基亚甲基环丙烷核苷是两种人类疱疹病毒 6（HHV-6）变体的有效抑制剂。我们研究了 HHV-6 U69 蛋白激酶在其作用机制中的作用。用纯化的 U69 对二羟甲基类似物环丙氟尿苷和单羟甲基核苷进行磷酸化，其中一个具有 6-醚部分（MBX 2168），另一个具有 6-硫醚部分（MBX 1616）。这三种化合物都是这种病毒激酶的底物，具有相似的米氏动力学参数。
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