首页> 外国专利> METHOD OF IDENTIFYING COMPOUNDS WHICH CAN ABOLISH THE BINDING INTERACTIONS BETWEEN THE VPR AND RIP-1 PROTEINS OF HIV-1

METHOD OF IDENTIFYING COMPOUNDS WHICH CAN ABOLISH THE BINDING INTERACTIONS BETWEEN THE VPR AND RIP-1 PROTEINS OF HIV-1

机译:鉴定可以消除HIV-1的VPR和RIP-1蛋白之间结合作用的化合物的方法

摘要

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.
机译:公开了一种治疗暴露于HIV或感染HIV的个体的方法,该方法包括给予所述个体治疗有效量的一种或多种化合物,所述化合物通过干扰由Vpr表达的Vpr的复制或其他基本功能来抑制或阻止所述HIV的复制。所述HIV,通过相互作用地阻断人细胞中的Vpr靶标,从而防止Vpr /靶标复合物从所述人细胞的细胞质转移至所述细胞核,其中Vpr进行HIV复制所必需的活性。在优选的实施方案中,一种或多种相互作用地阻断靶标的化合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,以及鉴定它们的方法和用于其中的试剂盒。

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