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New Service to Support the Development of Novel Deubiquitylase (DUB) Enzyme Inhibitors Launched

机译：支持新型Deubiquitylase（DUB）酶抑制剂的开发的新服务

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摘要

Ubiquigent Ltd has announced the launch of an exciting new service as part of its Drug Discovery Screening Platform - DUBprofiler-Cell. DUBprofiler-Cell supports the development of novel deubiquitylase (DUB) enzyme inhibitors by revealing the 'active DUBome' in a given cell-line or tissue (e.g. non-diseased and diseased), and by reporting the target engagement of test compounds to that 'active DUBome'. The DUBprofiler-Cell assay utilises activity-based probes to capture active DUBs (i.e. DUBs with reactive catalytic site cysteine residues) within a cell-line or tissue. By pre-incubating lysates or live cells with test compounds, the assay can be used to evaluate target engagement by compounds. This powerful approach allows proteins to be assayed under physiological conditions (e.g. use of a relevant cell line or tissue; proteins at endogenous expression levels and with a natural assembly and modification status) and is a valuable complementary method to build upon data from our comprehensive in vitro DUBprofiler service utilising recombinant DUB enzymes. Proof of concept validation of the assay has been demonstrated using potent covalent or non-covalent mechanisms of action selective inhibitors of USP7 or USP30; targets of significant interest in oncology and neurodegeneration, respectively. Other DUBs can be targeted using DUBprofiler-Cell as required.
机译：乌比伊特有限公司宣布推出令人兴奋的新服务作为其药物发现筛选平台的一部分 - Dubprofiler-Cell。 DUBPROFILER-CELL通过揭示给定的细胞系或组织（例如未患病和患病）的“活性大豆”，并通过将测试化合物的目标接合报告对该“有效的八方'。 Dubprofiler-Cell测定利用基于活性的探针在细胞系或组织内捕获活性配音（具有反应性催化位点残留物）的活性配音。通过用测试化合物预孵育裂解物或活细胞，可以使用测定来评估通过化合物的靶接合。这种强大的方法允许在生理条件下进行测定（例如，使用相关的细胞系或组织;内源性表达水平的蛋白质和自然组装和修饰状态），并且是我们全面的数据建立有价值的互补方法使用重组配音酶的体外DubProfiler服务。使用USP7或USP30的效果选择性抑制剂的有效的共价或非共价机制证明了测定概念验证的证据;分别对肿瘤和神经变性的重大兴趣的目标。其他配音可以根据需要使用DubProfiler-Cell定位。

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