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    Surrogate genetics target characterization method
    1.
    发明授权
    Surrogate genetics target characterization method 失效
    代理遗传学目标表征方法

    公开(公告)号：US06322973B1

    公开(公告)日：2001-11-27

    申请号：US09187918

    申请日：1998-11-06

    申请人： Keith Bostian ,  Georges Natsoulis

    发明人： Keith Bostian ,  Georges Natsoulis

    IPC分类号： C12Q168

    CPC分类号： C12N15/1079 ,  C12Q1/025 ,  C12Q1/6897

    摘要： A two-step, scalable method is described for identifying the cellular function(s) of one or more genes of unknown function, and for identifying modulators of the gene(s). The method uses the reversal or alteration of a phenotype created by the expression of the heterologous gene, e.g., a human gene, to identify modulators of that gene's activity. That modulator is then used in an in vitro or in vivo disease model system to identify compounds which affect disease progression. The subset of compounds which influence disease in a therapeutic manner are drug leads. However, all compounds which influence disease progression are tools to at least partially characterize gene function. The inhibitor identification step of the method is preferably carried out using a plurality of microbial strains or cell lines expressing different heterologous DNA sequences in a single solution. The method is particularly useful for genes which have not been validated as good inhibitor targets.

    摘要翻译： 描述了用于鉴定一个或多个未知功能基因的细胞功能以及用于鉴定基因调节剂的两步可扩展方法。 该方法使用通过异源基因（例如人基因）的表达产生的表型的逆转或改变来鉴定该基因活性的调节剂。 然后将该调节剂用于体外或体内疾病模型系统中以鉴定影响疾病进展的化合物。 以治疗方式影响疾病的化合物的子集是药物导向。 然而，影响疾病进展的所有化合物是至少部分表征基因功能的工具。 该方法的抑制剂鉴定步骤优选使用在单个溶液中表达不同异源DNA序列的多个微生物菌株或细胞系来进行。 该方法对于尚未被证实为良好抑制剂靶的基因特别有用。

    Enhancement of tigecycline potency using efflux pump inhibitors
    4.
    发明授权
    Enhancement of tigecycline potency using efflux pump inhibitors 失效
    使用外排泵抑制剂增强替加环素效力

    公开(公告)号：US07879795B2

    公开(公告)日：2011-02-01

    申请号：US11832626

    申请日：2007-08-01

    申请人： Tomasz Glinka ,  Keith Bostian ,  Olga Lomovskaya ,  Mark Surber ,  Dongxu Sun

    发明人： Tomasz Glinka ,  Keith Bostian ,  Olga Lomovskaya ,  Mark Surber ,  Dongxu Sun

    IPC分类号： A61K38/00

    CPC分类号： A61K31/165 ,  A61K31/426 ,  A61K31/433 ,  A61K31/47 ,  A61K31/65

    摘要： Disclosed herein are Efflux Pump Inhibitor (EPI) compounds that can be co-administered with antimicrobial agents for the treatment of infections caused by drug resistant pathogens. The EPI compounds are soft drugs which exhibit a reduced propensity for tissue accumulation. It is demonstrated that the EPIs can be used to increase the potency, decrease bacterial resistance and development of bacterial resistance, and increase killing effectivness of tigecycline. Also disclosed are methods of treatment and pharmaceutical compositions for co-administering tigecylcine with an EPI.

    摘要翻译： 本文公开了可与抗微生物剂共同施用以治疗由耐药性病原体引起的感染的流出泵抑制剂（EPI）化合物。 EPI化合物是表现出组织积累倾向降低的软性药物。 证明EPI可用于增加效力，降低细菌耐药性和细菌耐药性的发展，并增加替加环素的杀伤效果。 还公开了治疗方法和药物组合物，用于与十二烷基苯共同施用EPI。