COMPOSITIONS AND METHODS FOR IDENTIFYING ENZYME AND TRANSPORT PROTEIN INHIBITORS
    4.
    发明申请
    COMPOSITIONS AND METHODS FOR IDENTIFYING ENZYME AND TRANSPORT PROTEIN INHIBITORS 有权
    用于鉴定酶和运输蛋白抑制剂的组合物和方法

    公开(公告)号:US20120071344A1

    公开(公告)日:2012-03-22

    申请号:US13239199

    申请日:2011-09-21

    申请人: Roland WOLKOWICZ

    发明人: Roland WOLKOWICZ

    摘要: The invention is directed to compositions, e.g., cell-based and multiplexed platforms, to screen for small molecule drugs that inhibit enzymes such as proteases, e.g., viral proteases, e.g., HIV proteases; and methods for making and using these compositions. The invention provides compositions and methods for identifying compositions, e.g., drug molecules, that can inhibit proteases, e.g., viral proteases such as HIV proteases. In alternative embodiments, the invention provides cell-based platforms or assays to screen for compositions, e.g., small molecules or drugs, that inhibit or modify the activity of enzymes such as calcium-dependent protein convertases involved in HIV envelope protein processing, including cleavage of the HIV gp160 envelope precursor, resulting in gp120 and gp41 envelope products. In one embodiment, the invention provides a cell-based or multiplexed platform for monitoring the activity of enzymes, e.g., proteases such as viral proteases.

    摘要翻译: 本发明涉及组合物,例如基于细胞的多重平台以筛选抑制酶的小分子药物,例如蛋白酶,例如病毒蛋白酶,例如HIV蛋白酶; 以及制备和使用这些组合物的方法。 本发明提供了用于鉴定可抑制蛋白酶例如HIV蛋白酶等病毒蛋白酶的组合物例如药物分子的组合物和方法。 在替代实施方案中,本发明提供基于细胞的平台或测定法,以筛选抑制或改变酶活性的组合物,例如小分子或药物,例如参与HIV包膜蛋白加工的钙依赖性蛋白质转化酶,包括切割 HIV gp160信封前体,导致gp120和gp41信封产品。 在一个实施方案中,本发明提供了用于监测酶(例如蛋白酶例如病毒蛋白酶)的活性的基于细胞或复用的平台。

    COMPOSITIONS AND METHODS FOR IDENTIFYING ENZYME AND TRANSPORT PROTEIN INHIBITORS
    9.
    发明申请
    COMPOSITIONS AND METHODS FOR IDENTIFYING ENZYME AND TRANSPORT PROTEIN INHIBITORS 有权
    用于鉴定酶和运输蛋白抑制剂的组合物和方法

    公开(公告)号:US20160083775A1

    公开(公告)日:2016-03-24

    申请号:US14838283

    申请日:2015-08-27

    发明人: Roland WOLKOWICZ

    摘要: The invention is directed to compositions, e.g., cell-based and multiplexed platforms, to screen for small molecule drugs that inhibit enzymes such as proteases, e.g., viral proteases, e.g., HIV proteases; and methods for making and using these compositions. The invention provides compositions and methods for identifying compositions, e.g., drug molecules, that can inhibit proteases, e.g., viral proteases such as HIV proteases. In alternative embodiments, the invention provides cell-based platforms or assays to screen for compositions, e.g., small molecules or drugs, that inhibit or modify the activity of enzymes such as calcium-dependent protein convertases involved in HIV envelope protein processing, including cleavage of the HIV gp160 envelope precursor, resulting in gp120 and gp41 envelope products. In one embodiment, the invention provides a cell-based or multiplexed platform for monitoring the activity of enzymes, e.g., proteases such as viral proteases.

    摘要翻译: 本发明涉及组合物,例如基于细胞的多重平台以筛选抑制酶的小分子药物,例如蛋白酶,例如病毒蛋白酶,例如HIV蛋白酶; 以及制备和使用这些组合物的方法。 本发明提供了用于鉴定可抑制蛋白酶例如HIV蛋白酶等病毒蛋白酶的组合物例如药物分子的组合物和方法。 在替代实施方案中,本发明提供基于细胞的平台或测定法,以筛选抑制或改变酶活性的组合物,例如小分子或药物,例如参与HIV包膜蛋白加工的钙依赖性蛋白质转化酶,包括切割 HIV gp160信封前体,导致gp120和gp41信封产品。 在一个实施方案中,本发明提供了用于监测酶(例如蛋白酶例如病毒蛋白酶)的活性的基于细胞或复用的平台。