硫酸化聚阴离子对1型人类免疫缺陷病毒核糖核酸酶H的抑制作用
Inhibition of human immunodeficiency virus type 1 RNase H by sulfated polyanions.
作者信息
Moelling K, Schulze T, Diringer H
机构信息
Max-Planck-Institut für Molekulare Genetik, Berlin, Federal Republic of Germany.
出版信息
J Virol. 1989 Dec;63(12):5489-91. doi: 10.1128/JVI.63.12.5489-5491.1989.
Abstract
The reverse transcriptase (RT) activity of human immunodeficiency virus type 1 and other retroviruses is closely associated with a hybrid-degrading RNase H activity which is essential for retroviral replication. We have analyzed the effect of sulfated polysaccharides on human immunodeficiency virus type 1 recombinant RT and RNase H activities in vitro. Heparin, dextran sulfates, and xylan polysulfate were found to be much more potent inhibitors of RNase H than of RT and exhibit 50% infective doses of 0.04 to 0.1 micrograms/ml (corresponding to 0.1 to 25 nM) which is up to 5,000-fold more efficient than that for RT. Inhibitors of RNase H activity are attractive as antiviral drugs.
摘要
1型人类免疫缺陷病毒及其他逆转录病毒的逆转录酶（RT）活性与一种杂交降解核糖核酸酶H（RNase H）活性密切相关，该活性对逆转录病毒复制至关重要。我们已经在体外分析了硫酸化多糖对1型人类免疫缺陷病毒重组RT和RNase H活性的影响。发现肝素、硫酸葡聚糖和木聚糖多硫酸盐对RNase H的抑制作用比对RT的抑制作用要强得多，其半数感染剂量为0.04至0.1微克/毫升（相当于0.1至25纳摩尔），比RT的效率高多达5000倍。RNase H活性抑制剂作为抗病毒药物很有吸引力。
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