Neyts J, De Clercq E
Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium.
Biochem Pharmacol. 1994 Jan 13;47(1):39-41. doi: 10.1016/0006-2952(94)90435-9.
Foremost among the acyclic nucleoside phosphonates currently pursued for their potential in the treatment of herpes and retrovirus infections are (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine (HPMPC) and 9-(2-phosphonylmethoxyethyl)adenine (PMEA). These compounds are as such taken up by the cells and then phosphorylated by cellular enzymes to their diphosphoryl derivatives HPMPCpp and PMEApp. The main target for the antiviral action of HPMPCpp and PMEApp is the viral DNA polymerase. Whereas PMEApp has been shown to interact as a DNA chain terminator with both retro- and herpes viruses, the mechanism by which HPMPCpp inhibits herpes viral DNA synthesis remains the subject of further study.
目前因其在治疗疱疹和逆转录病毒感染方面的潜力而被研究的无环核苷膦酸盐中，最重要的是（S）-1-（3-羟基-2-膦酰甲氧基丙基）胞嘧啶（HPMPC）和9-（2-膦酰甲氧基乙基）腺嘌呤（PMEA）。这些化合物被细胞摄取后，再由细胞内的酶磷酸化为其二磷酸衍生物HPMPCpp和PMEApp。HPMPCpp和PMEApp抗病毒作用的主要靶点是病毒DNA聚合酶。虽然PMEApp已被证明可作为DNA链终止剂与逆转录病毒和疱疹病毒相互作用，但HPMPCpp抑制疱疹病毒DNA合成的机制仍有待进一步研究。
