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    • 5. 发明授权
    • Multimerization of HIV-1 Vif protein as a therapeutic target
    • HIV-1 Vif蛋白多聚化作为治疗靶点
    • US07226741B2
    • 2007-06-05
    • US10688100
    • 2003-10-17
    • Hui ZhangRoger J. PomerantzBin Yang
    • Hui ZhangRoger J. PomerantzBin Yang
    • C12Q1/68
    • C07K14/005A61K38/00C12N2740/16322Y10S530/826
    • One approach to treating individuals infected with HIV-1 is to administer to such individuals compounds that directly interfere with and intervene in the machinery by which HIV-1 replicates itself within human cells. Although the specific role of HIV-1 viral protein Vif in the viral life cycle is not known, the vif gene is essential for the pathogenic replication of lentiviruses in vivo. The present invention relates to a method for treating an individual exposed to or infected with HIV-1. Individuals identified as being exposed to or infected by HIV-1 are administered a therapeutically effective amount of one or more compounds that inhibit or prevent replication of said HIV-1 by interfering with the replicative or other essential functions of HIV-1 viral protein Vif by interactively blocking the multimerization domain of Vif, thereby preventing multimerization of Vif protein, which is important for Vif function in the lentivirus life cycle. In preferred embodiments, the compound or compounds that interactively block the multimerization domain of Vif are Vif antagonists. Pharmaceutical compositions comprising these compounds are also disclosed.
    • 治疗感染HIV-1的个体的一种方法是向这些个体施用直接干扰和干预HIV-1在人细胞内自身复制的机制的化合物。 虽然HIV-1病毒蛋白Vif在病毒生命周期中的具体作用尚不清楚,但vif基因对于体内慢病毒的致病性复制至关重要。 本发明涉及用于治疗暴露于或感染HIV-1的个体的方法。 被鉴定为暴露于HIV-1或感染HIV-1的个体通过干扰HIV-1病毒蛋白Vif的复制或其它基本功能来抑制或阻止所述HIV-1复制的治疗有效量的一种或多种化合物 交互阻断Vif的多聚化结构域,从而阻止Vif蛋白的多聚化,这对于慢病毒生命周期中的Vif功能是重要的。 在优选的实施方案中,交互式阻断Vif的多聚化结构域的化合物是Vif拮抗剂。 还公开了包含这些化合物的药物组合物。
    • 6. 发明授权
    • Multimerization of HIV-1 Vif protein as a therapeutic target
    • HIV-1 Vif蛋白多聚化作为治疗靶点
    • US06653443B2
    • 2003-11-25
    • US10118575
    • 2002-04-08
    • Hui ZhangRoger J. PomerantzBin Yang
    • Hui ZhangRoger J. PomerantzBin Yang
    • A61K3804
    • C07K14/005A61K38/00C12N2740/16322Y10S530/826
    • One approach to treating individuals infected with HIV-1 is to administer to such individuals compounds that directly interfere with and intervene in the machinery by which HIV-1 replicates itself within human cells. Although the specific role of HIV-1 viral protein Vif in the viral life cycle is not known, the vif gene is essential for the pathogenic replication of lentiviruses in vivo. The present invention relates to a method for treating an individual exposed to or infected with HIV-1. Individuals identified as being exposed to or infected by HIV-1 are administered a therapeutically effective amount of one or more compounds that inhibit or prevent replication of said HIV-1 by interfering with the replicative or other essential functions of HIV-1 viral protein Vif, by interactively blocking the multimerization domain of Vif, thereby preventing multimerization of Vif protein, which is important for Vif function in the lentivirus life cycle. In preferred embodiments, the compound or compounds that interactively block the multimerization domain of Vif are Vif antagonists. Pharmaceutical compositions comprising these compounds are also disclosed.
    • 治疗感染HIV-1的个体的一种方法是向这些个体施用直接干扰和干预HIV-1在人细胞内自身复制的机制的化合物。 虽然HIV-1病毒蛋白Vif在病毒生命周期中的具体作用尚不清楚,但vif基因对于体内慢病毒的致病性复制至关重要。 本发明涉及用于治疗暴露于或感染HIV-1的个体的方法。 鉴定为暴露于HIV-1或感染HIV-1的个体被施用治疗有效量的一种或多种化合物,其通过干扰HIV-1病毒蛋白Vif的复制或其它基本功能来抑制或阻止所述HIV-1的复制, 通过交互阻断Vif的多聚化结构域,从而防止Vif蛋白的多聚化,这对于慢病毒生命周期中的Vif功能是重要的。 在优选的实施方案中,交互式阻断Vif的多聚化结构域的化合物是Vif拮抗剂。 还公开了包含这些化合物的药物组合物。