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    Methods and formulations comprising agonists and antagonists of nuclear hormone receptors
    3.
    发明申请
    Methods and formulations comprising agonists and antagonists of nuclear hormone receptors 审中-公开
    包含核激素受体的激动剂和拮抗剂的方法和制剂

    公开(公告)号：US20060035813A1

    公开(公告)日：2006-02-16

    申请号：US10530254

    申请日：2003-10-03

    申请人： Esther Sternberg ,  Jeannette Webster ,  Leonardo Tonelli ,  Stephen Leppla ,  Mahtab Moayeri

    发明人： Esther Sternberg ,  Jeannette Webster ,  Leonardo Tonelli ,  Stephen Leppla ,  Mahtab Moayeri

    IPC分类号： A61K38/28

    CPC分类号： C07K14/005 ,  A61K38/164 ,  A61K38/4886 ,  C07K14/721 ,  C12N2740/16322 ,  C12Q1/6897 ,  G01N33/5044 ,  G01N33/743 ,  G01N33/78 ,  G01N2333/70567 ,  G01N2333/726 ,  Y02A50/469

    摘要： Novel compounds, pharmaceutical compositions, and methods are provided for modulating processes mediated by nuclear hormone receptors. A partial or complete agonist or antagonist modulates, directly or indirectly, an activity of one or more nuclear hormone receptors for glucocorticoids (GRs), androgens (ARs), mineralocorticoids (MRs), progestins (PRs), estrogens (ERs), thyroid hormones (TRs), vitamin D (VDRs), retinoids (RARs and RXRs), peroxisomes (XPARs and PPARs), icosanoids (IRs), or one or more orphan receptors, such as steroid and thyroid receptors. Exemplary compounds of the disclosure are bacterial products, for example bacterial toxins, and these compounds are useful in screens for other antagonists and agonists. Related methods and compositions are provided for diagnosis, treatment and prevention of bacterial disease and associated or unrelated inflammatory, autoimmune, toxic (including shock), and chronic and/or lethal sequelae associated with bacterial infection.

    摘要翻译： 提供新的化合物，药物组合物和方法用于调节由核激素受体介导的过程。 部分或完全激动剂或拮抗剂直接或间接调节一种或多种核激素受体对糖皮质激素（GR），雄激素（AR），盐皮质激素（MR），孕激素（PR）），雌激素（ER），甲状腺激素 （TRs），维生素D（VDR），类维生素A（RARs和RXR），过氧化物酶体（XPARs和PPARs），二十烷酸（IRs）或一种或多种孤儿受体，如类固醇和甲状腺受体。 本公开的示例性化合物是细菌产物，例如细菌毒素，并且这些化合物可用于其它拮抗剂和激动剂的筛选。 提供相关方法和组合物用于诊断，治疗和预防细菌性疾病和相关或不相关的炎性，自身免疫性，毒性（包括休克）以及与细菌感染相关的慢性和/或致死性后遗症。

    Imaging the activity of extracellular protease in cells using mutant anthrax toxin protective antigens that are cleaved by specific extracellular proteases
    6.
    发明申请
    Imaging the activity of extracellular protease in cells using mutant anthrax toxin protective antigens that are cleaved by specific extracellular proteases 审中-公开
    使用由特异性细胞外蛋白酶切割的突变炭疽毒素保护性抗原，在细胞中成像细胞外蛋白酶的活性

    公开(公告)号：US20050123476A1

    公开(公告)日：2005-06-09

    申请号：US10488806

    申请日：2002-09-05

    申请人： Thomas Bugge ,  Stephen Leppla ,  Shi-Hui Liu ,  David Mitola

    发明人： Thomas Bugge ,  Stephen Leppla ,  Shi-Hui Liu ,  David Mitola

    IPC分类号： A61K49/00 ,  A61K49/16 ,  A61K51/00 ,  A61K51/10 ,  C12Q1/37

    CPC分类号： A61K49/16 ,  A61K51/1009 ,  C12Q1/37 ,  G01N2500/02

    摘要： This invention pertains to methods for imaging the activity of extracellular proteases in cells using the anthrax binary toxin-system to target cells expressing extracellular proteases with mutant anthrax toxin protective antigens (μPrAg) that bind to receptors on the cells and are cleaved by a specific extracellular protease expressed by the cells, and ligands that specifically bind to the cleaved μPrAg and are linked to a moiety that is detectable by an imaging procedure. The μPrAg proteins used in the methods comprise a protease cleavage site that is cleaved by a specific extracellular protease and is in place of the furin cleavage site of the native PrAg. The methods are useful for diagnosing and treating diseases and undesirable physiological conditions correlated with the activity of extracellular proteases, and for optimizing the therapeutic efficacy of drugs used to treat such diseases and conditions.

    摘要翻译： 本发明涉及使用炭疽二元毒素系统对细胞外蛋白酶活性进行成像的方法，以靶向表达细胞外蛋白酶的细胞，所述突变体具有与细胞上的受体结合的突变炭疽毒素保护性抗原（muPrAg），并被细胞外特异性切割 由细胞表达的蛋白质，以及与切割的muPrAg特异性结合并与通过成像程序可检测的部分连接的配体。 用于该方法的muPrAg蛋白质包含由特异性细胞外蛋白酶切割并代替天然PrAg的弗林蛋白酶切割位点的蛋白酶切割位点。 该方法可用于诊断和治疗与细胞外蛋白酶活性相关的疾病和不良生理条件，并且用于优化用于治疗这些疾病和病症的药物的治疗功效。