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    • 23. 发明授权
    • Methods and compositions for inhibiting HIV replication
    • 用于抑制HIV复制的方法和组合物
    • US5780220A
    • 1998-07-14
    • US382873
    • 1995-02-03
    • David B. WeinerYosef RefaeliDavid N. Levy
    • David B. WeinerYosef RefaeliDavid N. Levy
    • A61K38/00C07K14/16C07K16/10C12P21/08G01N33/569C12Q1/70A01N43/04A61K31/56G01N33/53
    • C07K14/005C07K16/1072G01N33/56988A61K38/00C12N2740/16322Y10S514/01
    • A method for treating an individual exposed to or infected with HIV is disclosed which comprises administering to said individual a therapeutically effective amount of one or more compounds which inhibit or prevent replication of said HIV by interfering with the replicative or other essential functions of Vpr expressed by said HIV, by interactively blocking the Vpr target in human cells, and thereby preventing translocation of the Vpr/target complex from the cytosol of said human cells to the nuclei of said cells, where Vpr carries on activities essential to replication of HIV. In preferred embodiments, the compound or compounds which interactively block the target are steroid hormone receptor antagonists, glucocorticoid receptor antagonists, or glucocorticoid receptor Type II antagonists, especially mifepristone (RU-486). Pharmaceutical compositions comprising these compounds, as well as a method for identifying them and a kit for use therein, are also disclosed.
    • 公开了一种用于治疗暴露于或感染HIV的个体的方法,其包括向所述个体施用治疗有效量的一种或多种化合物,所述一种或多种化合物通过干扰由Vpr表达的Vpr的复制或其它基本功能来抑制或阻止所述HIV的复制 所述HIV通过交互阻断人细胞中的Vpr靶,从而防止Vpr /靶复合物从所述人细胞的胞质溶胶转移到所述细胞的细胞核,其中Vpr进行HIV复制必需的活性。 在优选的实施方案中,交互地阻断靶标的化合物或类似物是类固醇激素受体拮抗剂,糖皮质激素受体拮抗剂或糖皮质激素受体II型拮抗剂,特别是米非司酮(RU-486)。 还公开了包含这些化合物的药物组合物,以及用于鉴定它们的方法和用于其中的试剂盒。