Compositions and methods for identifying enzyme and transport protein inhibitors
    2.
    发明授权
    Compositions and methods for identifying enzyme and transport protein inhibitors 有权
    用于鉴定酶和转运蛋白抑制剂的组合物和方法

    公开(公告)号:US09518254B2

    公开(公告)日:2016-12-13

    申请号:US13266777

    申请日:2010-05-03

    申请人: Roland Wolkowicz

    发明人: Roland Wolkowicz

    摘要: The invention is directed to compositions to screen for small molecule drugs that inhibit proteases, such as 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., HIV proteases. In alternative embodiments, the invention provides cell-based 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 envelop protein processing, including cleavage of the HIV gp160 envelope precursor, resulting in gp120 and gp41 envelope products.

    摘要翻译: 本发明涉及筛选抑制蛋白酶的小分子药物的组合物,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。 本发明提供用于鉴定可抑制蛋白酶例如HIV蛋白酶的组合物的组合物和方法,例如药物分子。 在替代实施方案中,本发明提供了基于细胞的测定法,以筛选抑制或改变酶活性的组合物,例如小分子或药物,所述酶例如涉及HIV包膜蛋白加工的钙依赖性蛋白质转化酶,包括HIV的切割 gp160信封前体,产生gp120和gp41信封产品。

    COMPOSITIONS AND METHODS FOR IDENTIFYING ENZYME AND TRANSPORT PROTEIN INHIBITORS
    3.
    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:US20120172253A1

    公开(公告)日:2012-07-05

    申请号:US13266777

    申请日:2010-05-03

    申请人: Roland Wolkowicz

    发明人: Roland Wolkowicz

    IPC分类号: C40B30/06 C07H21/04 C12Q1/68

    摘要: The invention is directed to compositions to screen for small molecule drugs that inhibit proteases, such as 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., HIV proteases. In alternative embodiments, the invention provides cell-based 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 envelop protein processing, including cleavage of the HIV gp160 envelope precursor, resulting in gp120 and gp41 envelope products.

    摘要翻译: 本发明涉及筛选抑制蛋白酶的小分子药物的组合物,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。 本发明提供用于鉴定可抑制蛋白酶例如HIV蛋白酶的组合物的组合物和方法,例如药物分子。 在替代实施方案中,本发明提供了基于细胞的测定法,以筛选抑制或改变酶活性的组合物,例如小分子或药物,所述酶例如涉及HIV包膜蛋白加工的钙依赖性蛋白质转化酶,包括HIV的切割 gp160信封前体,产生gp120和gp41信封产品。

    Immunogenic compositions for induction of anti-tumor immunity
    4.
    发明授权
    Immunogenic compositions for induction of anti-tumor immunity 失效
    用于诱导抗肿瘤免疫的免疫原性组合物

    公开(公告)号:US07378092B2

    公开(公告)日:2008-05-27

    申请号:US11129359

    申请日:2005-05-16

    IPC分类号: A61K39/395 A61K39/00

    摘要: The invention relates to methods of inducing an anti-tumor immunity and/or inducing an immune responses to p53 in mammals. The methods comprise administering to a mammal an effective amount of at least one immunogen selected from the group consisting of: (i) a peptide based on a CDR of the heavy or light chain of an anti-p53 mAb, which peptide is capable of eliciting antibodies to p53; and (ii) a DNA molecule coding for the variable (V) region of an anti-p53 mAb in a suitable gene delivery vehicle. Preferably the immunogen is administered in the form of a pharmaceutical composition. Preferably the peptide is 7 to 30 amino acid residues in length and contains a sequence of the CDR2 or CDR3 of the heavy chain, or of the CDR3 of the light chain of an anti-p53 mAb.

    摘要翻译: 本发明涉及在哺乳动物中诱导抗肿瘤免疫和/或诱导对p53的免疫应答的方法。 所述方法包括向哺乳动物施用有效量的选自以下的至少一种免疫原:(i)基于抗p53mAb的重链或轻链的CDR的肽,所述肽能够引发 p53抗体; 和(ii)在合适的基因递送载体中编码抗p53mAb的可变(V)区的DNA分子。 优选地,免疫原以药物组合物的形式施用。 优选地,肽的长度为7至30个氨基酸残基,并且含有重链的CDR2或CDR3的序列,或抗-p53mAb的轻链的CDR3的序列。

    Immunogenic compositions for induction of anti-tumor immunity
    5.
    发明申请
    Immunogenic compositions for induction of anti-tumor immunity 失效
    用于诱导抗肿瘤免疫的免疫原性组合物

    公开(公告)号:US20050208065A1

    公开(公告)日:2005-09-22

    申请号:US11129359

    申请日:2005-05-16

    摘要: The invention relates to methods of inducing an anti-tumor immunity and/or inducing an immune responses to p53 in mammals. The methods comprise administering to a mammal an effective amount of at least one immunogen selected from the group consisting of: (i) a peptide based on a CDR of the heavy or light chain of an anti-p53 mAb, which peptide is capable of eliciting antibodies to p53; and (ii) a DNA molecule coding for the variable (V) region of an anti-p53 mAb in a suitable gene delivery vehicle. Preferably the immunogen is administered in the form of a pharmaceutical composition. Preferably the peptide is 7 to 30 amino acid residues in length and contains a sequence of the CDR2 or CDR3 of the heavy chain, or of the CDR3 of the light chain of an anti-p53 mAb.

    摘要翻译: 本发明涉及在哺乳动物中诱导抗肿瘤免疫和/或诱导对p53的免疫应答的方法。 所述方法包括向哺乳动物施用有效量的选自以下的至少一种免疫原:(i)基于抗p53mAb的重链或轻链的CDR的肽,所述肽能够引发 p53抗体; 和(ii)在合适的基因递送载体中编码抗p53mAb的可变(V)区的DNA分子。 优选地,免疫原以药物组合物的形式施用。 优选地,肽的长度为7至30个氨基酸残基并且包含重链的CDR2或CDR3的序列或抗p53mAb的轻链的CDR3的序列。

    Compositions and methods for identifying enzyme and transport protein inhibitors
    6.
    发明授权
    Compositions and methods for identifying enzyme and transport protein inhibitors 有权
    用于鉴定酶和转运蛋白抑制剂的组合物和方法

    公开(公告)号:US09169312B2

    公开(公告)日:2015-10-27

    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。

    IMMUNOGENIC COMPOSITIONS FOR INDUCTION OF ANTI-TUMOR IMMUNITY
    7.
    发明申请
    IMMUNOGENIC COMPOSITIONS FOR INDUCTION OF ANTI-TUMOR IMMUNITY 审中-公开
    免疫组织化学诱导抗肿瘤免疫

    公开(公告)号:US20090098116A1

    公开(公告)日:2009-04-16

    申请号:US11943255

    申请日:2007-11-20

    IPC分类号: A61K39/395 A61K31/711

    摘要: The invention relates to the use of an immunogen selected from the group consisting of(i) an anti-p53 mAb;(ii) a fragment of an anti-p53 mAb;(iii) a peptide based on a CDR of the heavy or light chain of an anti-p53 mAb, which peptide is capable of eliciting antibodies to p53; and(iv) a DNA molecule coding for the variable (V) region of an anti-p53 mAb in a suitable gene delivery vehicle,for the preparation of a pharmaceutical composition useful for induction of anti-tumor immunity in mammals, for activating an enhanced immune response to a p53 molecule in mammals, and/or for induction of immune responses to mutated and wild-type forms of a p53 in mammals. The use of anti-p53 mAbs and novel peptides based on the CDR2 and CDR3 of the heavy chains and CDR3 of the light chains of different anti-p53 mAbs are disclosed.

    摘要翻译: 本发明涉及选自以下的免疫原的用途:(i)抗p53 mAb; (ii)抗p53 mAb的片段; (iii)基于抗p53 mAb的重链或轻链的CDR的肽,该肽能够引发针对p53的抗体; 和(iv)编码合适的基因递送载体中抗p53mAb的可变(V)区的DNA分子,用于制备用于诱导哺乳动物抗肿瘤免疫的药物组合物,用于激活增强的 对哺乳动物中p53分子的免疫应答,和/或用于诱导哺乳动物中突变​​和野生型形式的p53的免疫应答。 公开了使用抗p53 mAb和基于不同抗p53 mAb的轻链的CDR2和CDR3的CDR3和新型肽。