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聚合酶底物耗竭:一种抑制人类免疫缺陷病毒复制的新策略。

Polymerase substrate depletion: a novel strategy for inhibiting the replication of the human immunodeficiency virus.

作者信息

Ichimura H, Levy J A

机构信息

Cancer Research Institute, University of California School of Medicine, San Francisco 94143, USA.

出版信息

Virology. 1995 Aug 20;211(2):554-60. doi: 10.1006/viro.1995.1437.

DOI:10.1006/viro.1995.1437
PMID:7544050
Abstract

Mycophenolic acid (MPA), an inhibitor of inosine monophosphate dehydrogenase, shows strong anti-HIV activity in vitro in both human peripheral blood CD4+ lymphocytes and macrophages, as well as established human cell lines. MPA shows its greatest antiviral effects during the early stages of HIV infection. By limiting the rate of de novo synthesis of guanosine nucleotides, this drug apparently blocks the activity of reverse transcriptase, which is required for the formation of the HIV DNA provirus. MPA provides a novel strategy for inhibiting the replication of HIV and should be considered in clinical trials of antiviral therapies.

摘要

霉酚酸(MPA)是肌苷单磷酸脱氢酶的抑制剂,在体外对人外周血CD4+淋巴细胞、巨噬细胞以及已建立的人细胞系均显示出强大的抗HIV活性。MPA在HIV感染的早期阶段显示出最大的抗病毒作用。通过限制鸟苷核苷酸的从头合成速率,这种药物显然阻断了逆转录酶的活性,而逆转录酶是HIV DNA前病毒形成所必需的。MPA为抑制HIV复制提供了一种新策略,应在抗病毒治疗的临床试验中予以考虑。

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