Cheng Y C, Grill S P, Dutschman G E, Nakayama K, Bastow K F
J Biol Chem. 1983 Oct 25;258(20):12460-4.
The metabolism of 9-(1,3-dihydroxy-2-propoxymethyl)guanine (DHPG), one of the most promising new anti-herpes virus compounds, in HeLa cells infected with herpes simplex virus type 1 was compared with that in the uninfected HeLa cells. In the virus-infected cells, the uptake of DHPG was enhanced and the major metabolites were found to be the mono-, di-, and triphosphate derivatives. The formation of these metabolites was dependent on the extracellular concentration of DHPG (0.5 to 5.0 microM). Virus-induced thymidine kinase was capable of phosphorylating DHPG to its monophosphate which could be further phosphorylated to the di- and triphosphate derivatives by the host cellular enzymes. Incorporation of the DHPG into DNA was observed in virus-infected cells. In contrast with 9-(2-hydroxyethoxymethyl)guanine, DHPG seemed not to serve as a chain terminator, but to be incorporated internally into DNA strands.
9-(1,3-二羟基-2-丙氧甲基)鸟嘌呤（DHPG）是最有前景的新型抗疱疹病毒化合物之一，对感染1型单纯疱疹病毒的HeLa细胞中DHPG的代谢与未感染的HeLa细胞中的代谢进行了比较。在病毒感染的细胞中，DHPG的摄取增强，主要代谢产物为单磷酸、二磷酸和三磷酸衍生物。这些代谢产物的形成取决于DHPG的细胞外浓度（0.5至5.0微摩尔）。病毒诱导的胸苷激酶能够将DHPG磷酸化为其单磷酸，该单磷酸可被宿主细胞酶进一步磷酸化为二磷酸和三磷酸衍生物。在病毒感染的细胞中观察到DHPG掺入DNA。与9-(2-羟乙氧甲基)鸟嘌呤不同，DHPG似乎不是链终止剂，而是在内部掺入DNA链中。
