SUMOYLATION OF SERCA2A AND CARDIOVASCULAR DISEASE
    26.
    发明公开
    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:EP2736516A1

    公开(公告)日:2014-06-04

    申请号:EP12811596.1

    申请日:2012-07-13

    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 SUMOl 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,例如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。 进一步提供了诊断发展为心力衰竭倾向的方法,包括确定SERCA2a突变体是否存在或确定SUMO1在心肌细胞中的表达水平。 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。

    FLUORESCENT -LABELLED DIUBIQUITIN SUBSTRATE FOR A DEUBIQUITINASE ASSAY
    28.
    发明公开
    FLUORESCENT -LABELLED DIUBIQUITIN SUBSTRATE FOR A DEUBIQUITINASE ASSAY 有权
    荧光标记的二硫苏糖酸底物用于DEUBIQUITIITINASE测定

    公开(公告)号:EP2580344A1

    公开(公告)日:2013-04-17

    申请号:EP11729135.1

    申请日:2011-06-14

    IPC分类号: C12Q1/37

    摘要: There is described a substrate for measuring the activity of a deubiquitinating enzyme (DUB), comprising a diubiquitin molecule, wherein an ubiquitin monomer is labeled with a fluorescent label, as well as an assay for DUB enzymes using such substrates.

    摘要翻译: 描述了用于测量脱遍在蛋白化酶(DUB)活性的底物,其包含二泛素分子,其中泛素单体用荧光标记物标记,以及使用这种底物的DUB酶测定法。

    Pharmacological profiling of drugs with cell-based assays
    29.
    发明公开
    Pharmacological profiling of drugs with cell-based assays 审中-公开
    Pharmakologische Profilierung von Arzneimitteln mit zellenbasierten Assays

    公开(公告)号:EP2341345A1

    公开(公告)日:2011-07-06

    申请号:EP10015839.3

    申请日:2005-08-18

    IPC分类号: G01N33/50 C12Q1/02

    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的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)将所述概况与具有确定的安全特征的药物的概况进行比较。 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,以及至少一种高含量测定法,其量为和 /或蛋白质 - 蛋白质相互作用的亚细胞位置。