Chan E W, Lee C K, Dale P J, Nortridge K R, Hom S S, Seed T M
J Gen Virol. 1981 Feb;52(Pt 2):291-9. doi: 10.1099/0022-1317-52-2-291.
Polyinosinic acids containing methyl and sulphur substitutions are potent inhibitors of reverse transcriptase. Substitution of sulphur for oxygen at the 6 position produces significant effects on the properties of polyinosinic acid: the kinetics of inhibition change from competitive to mixed-type and the inhibition constant falls by three orders of magnitude. In contrast, 1-methyl substitution produces no such effects. Poly(1-methyl-6-thioinosinic acid) or poly(m1s6I) inhibits irreversibly, inhibiting all ten reverse transcriptases tested under a variety of assay conditions. In cell culture test systems, poly(m1s6I) is capable of blocking both infection by non-transforming viruses and transformation by a sarcoma virus. The presence of poly(m1s6I) in a preinfected culture results in the production of non-infectious virus particles lacking reverse transcriptase activity.
含有甲基和硫取代基的聚肌苷酸是逆转录酶的有效抑制剂。在6位用硫取代氧对聚肌苷酸的性质产生显著影响：抑制动力学从竞争性变为混合型，抑制常数下降三个数量级。相比之下，1-甲基取代没有产生这样的影响。聚（1-甲基-6-硫代肌苷酸）或聚（m1s6I）不可逆地抑制，在各种测定条件下抑制所测试的所有十种逆转录酶。在细胞培养测试系统中，聚（m1s6I）能够阻断非转化病毒的感染和肉瘤病毒的转化。在预感染培养物中存在聚（m1s6I）会导致产生缺乏逆转录酶活性的非感染性病毒颗粒。
