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    ADENYLATION ENZYME INHIBITORS
    34.
    发明申请
    ADENYLATION ENZYME INHIBITORS 审中-公开
    腺嘌呤抑制剂

    公开(公告)号：WO2016032332A1

    公开(公告)日：2016-03-03

    申请号：PCT/NL2015/050596

    申请日：2015-08-26

    申请人： STICHTING HET NEDERLANDS KANKER INSTITUUT - ANTONI VAN LEEUWENHOEK ZIEKENHUIS

    发明人： OVAA, Huib ,  EL OUALID, Farid ,  MULDER, Monique

    IPC分类号： A61K38/00

    CPC分类号： C07K14/4702 ,  A61K38/00 ,  C07K7/06 ,  C12N9/93 ,  C12N9/99 ,  C12Q1/25 ,  C12Q1/48 ,  C12Y203/02 ,  C12Y603/02019 ,  G01N33/581 ,  G01N2333/9015 ,  G01N2333/9108 ,  G01N2440/40

    摘要： The present invention concerns compounds that are capable of covalently entrapping adenylatingenzymes. The present inventionis essentially based on the discovery that analogues of adenylating enzyme (AE) substrates, wherein a methylene group has been incorporated at the carbon atom in the α-position relative to the carboxylate group involved in the adenylation, are capable of undergoing the adenylation reaction, thereby creating an activated methylene group in situ. The resulting 'armed' acyladenylate can interact with the enzyme resulting in covalent entrapment. Interestingly, the acyladenylate can alternatively be transferredto the next step in the enzyme cascade, followingwhich the activated methylene group can interact with thenext(active site cysteine containing) enzyme in theenzymatic cascade. The AE substrate analogues, based on their capability of 'entrapping' the respective enzymes, will have utility as activity based probes in biological research and also as diagnostic and/or therapeutic agents.

    摘要翻译： 本发明涉及能够共价捕获腺苷酸化酶的化合物。 本发明基本上是基于以下发现：相对于涉及腺苷酸化的羧酸酯基，已经在相对于α位置的碳原子处并入亚甲基化酶（AE）底物的类似物能够进行腺苷酸化 反应，从而在原位产生活化的亚甲基。 所产生的“武装”酰基腺苷酸可与酶相互作用，导致共价捕获。 有趣的是，酰基腺苷酸可以替代地转移到酶级联中的下一步骤，随后活化的亚甲基可以在酶切级联中与当前的（活性位点半胱氨酸）酶相互作用。 AE底物类似物基于其夹带各自酶的能力，将作为生物研究中的基于活性的探针以及诊断和/或治疗剂具有实用性。

    INJECTION DEVICE, INJECTION ASSEMBLY AND MONITORING DEVICE.
    39.
    发明申请
    INJECTION DEVICE, INJECTION ASSEMBLY AND MONITORING DEVICE. 审中-公开

    公开(公告)号：WO2023022596A1

    公开(公告)日：2023-02-23

    申请号：PCT/NL2022/050476

    申请日：2022-08-19

    申请人： STICHTING HET NEDERLANDS KANKER INSTITUUT-ANTONI VAN LEEUWENHOEK ZIEKENHUIS

    发明人： BLANK, Christian Ulrich ,  LIJNSVELT, Judith Marjan

    IPC分类号： A61M5/142 ,  A61M5/172 ,  A61B5/145

    摘要： A monitoring device for monitoring a hypocortiolism patient, the monitoring device comprising: - a needle for penetrating a skin of the patient, and - an analysis module fluidly connected with the needle, the analysis module comprising: o a first sensor, for measuring an inflammation level representative for the patient; and/or o a second sensor, for measuring a stress level representative for the patient; and wherein the monitoring device is configured to automatically trigger a notification in response to the first sensor measuring an inflammation level exceeding a first pre-defined threshold and/or in response to the second sensor measuring a stress level exceeding a second pre-defined threshold.