卡波韦、齐多夫定和三磷酸双脱氧核苷对人类免疫缺陷病毒逆转录酶及所选人类聚合酶活性影响的比较。
Comparison of the effect of Carbovir, AZT, and dideoxynucleoside triphosphates on the activity of human immunodeficiency virus reverse transcriptase and selected human polymerases.
作者信息
White E L, Parker W B, Macy L J, Shaddix S C, McCaleb G, Secrist J A, Vince R, Shannon W M
机构信息
Kettering-Meyer Laboratory, Southern Research Institute, Birmingham, AL 35255.
出版信息
Biochem Biophys Res Commun. 1989 Jun 15;161(2):393-8. doi: 10.1016/0006-291x(89)92611-9.
Carbocylic 2',3'-didehydro-2',3'-dideoxyguanosine (Carbovir; NSC 614846) is an antiretroviral agent which may be useful in the treatment of AIDS. We have synthesized the 5'-triphosphate of Carbovir and examined its ability to inhibit human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (EC 2.7.7.49) and other retroviral reverse transcriptases, as well as human DNA polymerases alpha, beta, gamma (EC 2.7.7.7) and DNA primase (EC 2.7.7.6). Carbovir triphosphate emerges as a highly selective inhibitor of reverse transcriptases with little, if any, effect on the cellular enzymes. 3'-Azido-2',3'-dideoxythymidine (AZT) triphosphate and the two dideoxynucleoside triphosphates, ddTTP and ddGTP, inhibited HIV-1 reverse transcriptase to the same degree as Carbovir triphosphate, but were less selective in that they also inhibited DNA polymerases beta and gamma. We conclude that Carbovir is a highly selective antiretroviral agent.
碳环2′,3′-二脱氢-2′,3′-二脱氧鸟苷（卡波韦；NSC 614846）是一种抗逆转录病毒药物，可能对治疗艾滋病有用。我们合成了卡波韦的5′-三磷酸酯，并检测了其抑制1型人类免疫缺陷病毒（HIV-1）逆转录酶（EC 2.7.7.49）和其他逆转录病毒逆转录酶以及人类DNA聚合酶α、β、γ（EC 2.7.7.7）和DNA引发酶（EC 2.7.7.6）的能力。卡波韦三磷酸酯是一种对逆转录酶具有高度选择性的抑制剂，对细胞酶几乎没有影响（如果有影响的话）。3′-叠氮-2′,3′-二脱氧胸苷（AZT）三磷酸酯以及两种双脱氧核苷三磷酸酯，即ddTTP和ddGTP，对HIV-1逆转录酶的抑制程度与卡波韦三磷酸酯相同，但选择性较差，因为它们也抑制DNA聚合酶β和γ。我们得出结论，卡波韦是一种高度选择性的抗逆转录病毒药物。
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