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    Pharmacological profiling of drugs with cell-based assays
    21.
    发明申请
    Pharmacological profiling of drugs with cell-based assays 审中-公开
    用基于细胞的测定法对药物进行药理学分析

    公开(公告)号：US20060040338A1

    公开(公告)日：2006-02-23

    申请号：US11205021

    申请日：2005-08-17

    申请人： John Westwick ,  Helen Yu ,  Marnie MacDonald

    发明人： John Westwick ,  Helen Yu ,  Marnie MacDonald

    IPC分类号： C12Q1/02 ,  C12M1/34

    CPC分类号： C12Q1/025 ,  G01N33/5023 ,  G01N33/5035 ,  G01N33/5041 ,  G01N33/5097 ,  G01N2440/00 ,  G01N2440/10 ,  G01N2440/12 ,  G01N2440/36 ,  G01N2440/38 ,  G01N2500/10

    摘要： The instant invention provides a method for establishing safety profiles for chemical compounds, as well as pharmacological profiling said method comprising (A) testing the effects of said chemical compounds on the amount and/or post-translational modifications of two or more macromolecules in intact cells; (B) constructing a pharmacological profile based on the results of said tests; and (C) comparing said profile to the profile(s) of drugs with established safety characteristics. Additionally, the invention is also directed to a composition comprising an assay panel, said panel comprising at least one high-content assay for the amount and/or post-translational modification of a protein and at least one high-content assay for the amount and/or subcellular location of a protein-protein interaction.

    摘要翻译： 本发明提供了一种用于建立化学化合物安全性的方法，以及药理学分析，所述方法包括（A）测试所述化合物对完整细胞中两种或更多种大分子的量和/或翻译后修饰的影响 ; （B）基于所述测试的结果构建药理学特征; 和（C）将所述外形与具有确定的安全特性的药物的特征进行比较。 此外，本发明还涉及包含测定面板的组合物，所述面板包含至少一种用于蛋白质的量和/或翻译后修饰的高含量测定法，以及至少一种高含量测定法，其量和/ /或蛋白质 - 蛋白质相互作用的亚细胞位置。

    Methods of identifying SENP1 inhibitors
    23.
    发明授权
    Methods of identifying SENP1 inhibitors 有权

    公开(公告)号：US09791447B2

    公开(公告)日：2017-10-17

    申请号：US14247153

    申请日：2014-04-07

    申请人： City of Hope

    发明人： Yuan Chen

    IPC分类号： G01N33/573

    CPC分类号： G01N33/573 ,  G01N2440/36 ,  G01N2500/02

    摘要： Provided herein are methods of detecting binding of an SENP1 polypeptide to a compound and methods for screening for inhibitors of SENP1. Further provided are aqueous compositions comprising SENP1 polypeptides and NMR apparatuses comprising the compositions for NMR analysis.

    METHODS FOR IDENTIFYING PROTEINS AND COMPOUNDS THAT MODULATE THE ACTIVITY OF OTUB1
    25.
    发明申请
    METHODS FOR IDENTIFYING PROTEINS AND COMPOUNDS THAT MODULATE THE ACTIVITY OF OTUB1 审中-公开
    用于鉴定调节OTUB1活性的蛋白质和化合物的方法

    公开(公告)号：US20160053298A1

    公开(公告)日：2016-02-25

    申请号：US14785429

    申请日：2014-04-14

    申请人： The Johns Hopkins University

    发明人： Cynthia Wolberger ,  Anthony Dibello ,  Reuven Wiener

    IPC分类号： C12Q1/37

    CPC分类号： C12Q1/37 ,  G01N2333/9015 ,  G01N2333/948 ,  G01N2440/36

    摘要： The present invention describes that OTUB1 cleavage of K48 poly-ubiquitin is stimulated by a select subset of E2 enzymes, and that this stimulation is regulated by the ubiquitin-charged state of the E2 and free ubiquitin. Structural and biochemical studies of OTUB1 and UBCH5B show that the E2 stimulates binding of the polyubiquitin substrate by contacting the OTUB1 N-terminal ubiquitin-binding helix. Methods for identifying E2 enzymes which stimulate or inhibit cleavage of K48 polyubiquitin, as well as novel target compounds which modulate this interaction are provided.

    摘要翻译： 本发明描述了通过E2酶的选择子集刺激K48多聚泛蛋白的OTUB1切割，并且该刺激受E2和免费泛蛋白的泛素充电状态的调节。 OTUB1和UBCH5B的结构和生物化学研究表明，E2通过接触OTUB1 N端泛素结合螺旋刺激多聚遍在蛋白底物的结合。 提供了用于鉴定刺激或抑制K48多聚遍在蛋白裂解的E2酶的方法，以及调节这种相互作用的新型靶化合物。

    Sumoylation of SERCA2a and Cardiovascular Disease
    29.
    发明申请
    Sumoylation of SERCA2a and Cardiovascular Disease 审中-公开
    SERCA2a和心血管疾病的协调

    公开(公告)号：US20150316551A1

    公开(公告)日：2015-11-05

    申请号：US14798357

    申请日：2015-07-13

    申请人： Roger Joseph Hajjar ,  Chang Won Kho ,  Ah Young Lee

    发明人： Roger Joseph Hajjar ,  Chang Won Kho ,  Ah Young Lee

    IPC分类号： G01N33/573 ,  C12Q1/68

    CPC分类号： A61K38/50 ,  A61K31/7088 ,  A61K38/1709 ,  A61K48/0066 ,  C12N7/00 ,  C12N15/86 ,  C12N2750/14143 ,  C12Q1/6883 ,  C12Q2600/136 ,  C12Q2600/158 ,  C12Y305/00 ,  G01N33/573 ,  G01N2333/914 ,  G01N2440/36 ,  G01N2800/325

    摘要： Methods for treating cardiovascular disease, and in particular heart failure, are provided comprising administering a therapeutically effective amount of a modulator of SERCA2a post-translation modification such as SUMOylation or acetylation. Also provided are methods of treating cardiovascular disease by inhibiting SERCA2a degradation. Further provided are methods of diagnosing a propensity to develop heart failure comprising determining if a SERCA2a mutant is present or determining the level of expression of SUMO1 in cardiomyocytes. The disclosure also provides methods of screening for therapeutics that modulate the post-translational modification of SERCA2a, such as by modulating post-translational SUMOylation and/or acetylation.

    摘要翻译： 提供了治疗心血管疾病，特别是心力衰竭的方法，包括施用治疗有效量的SERCA2a翻译后修饰调节剂如SUMO化或乙酰化。 还提供了通过抑制SERCA2a降解来治疗心血管疾病的方法。 进一步提供诊断心力衰竭发展倾向的方法，包括确定是否存在SERCA2a突变体或确定心肌细胞中SUMO1的表达水平。 本公开还提供筛选调节SERCA2a的翻译后修饰的治疗剂的方法，例如通过调节翻译后SUMO化和/或乙酰化。

    Detection and quantification of modified proteins
    30.
    发明授权
    Detection and quantification of modified proteins 有权
    修饰蛋白的检测和定量

    公开(公告)号：US08669116B2

    公开(公告)日：2014-03-11

    申请号：US10506877

    申请日：2003-03-11

    申请人： Steven P. Gygi ,  Junmin Peng

    发明人： Steven P. Gygi ,  Junmin Peng

    IPC分类号： C12Q1/37 ,  C07K1/22 ,  G01N33/68

    CPC分类号： G01N33/6848 ,  C07K1/22 ,  C07K7/08 ,  C12Q1/37 ,  G01N33/6803 ,  G01N33/6842 ,  G01N33/6896 ,  G01N2440/36 ,  G01N2560/00 ,  Y10T436/24

    摘要： The invention provides a method detecting and quantifying proteins by mass spectrophotometric analysis using peptide internal standards and provides a highly sensitive way of detecting protein modifications. In one aspect, the invention provides a method for determining a site of ubiquitination in a polypeptide and for evaluating ubiquitination targets in a population of polypeptides. In this way, a proteome ubiquitination map can be obtained which comprises information relating to the ubiquitination states of a plurality of cellular polypeptides. Maps can be obtained for a variety of different types of cells and cell states. For example, ubiquitination targets in normal and diseased cells can be evaluated. Preferably, the map is stored as data files in a database. Individual ubiquitinated polypeptides identified can be used to generate molecular probes diagnostic of a cell state and/or can serve as targets for agents that modulate one or more cellular processes.

    摘要翻译： 本发明提供了通过使用肽内标的质谱分析法检测和定量蛋白质的方法，并提供了检测蛋白质修饰的高度灵敏的方法。 一方面，本发明提供了一种确定多肽泛素化位点的方法，并用于评价多肽群体中的泛素化靶标。 以这种方式，可以获得包含与多个细胞多肽的泛素化状态有关的信息的蛋白质组泛素化图。 可以获得各种不同类型的细胞和细胞状态的图。 例如，可以评估正常和患病细胞中的泛素化靶标。 优选地，地图作为数据文件存储在数据库中。 鉴定的单个泛素化多肽可用于产生诊断细胞状态的分子探针和/或可用作调节一种或多种细胞过程的试剂的靶标。