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NOVEL PHARMACEUTICALLY ACTIVE COMPOUNDS INTERACTING WITH GTP-BINDING PROTEINS

机译：与GTP结合蛋白相互作用的新型药物活性化合物

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摘要

The present invention relates to compounds that bind to the surface of normal or mutated GTP binding proteins and reduce the activation energy of the GTPase activity thereof by introduction of at least one functional group into the active site of said proteins. Said compounds are of synthetic or semi-synthetic origin. Preferably, the functional group referred to above is an arginine finger or a derivative thereof or a compound that mimics the activity of an arginine finger that is obtained, for example, by peptidomimetics. The invention further relates to a pharmaceutical composition comprising the compound of the invention as well as to methods for treating patients suffering from oncogenic activations of Ras genes, from tumors caused by malfunction of G proteins or from neurofibromatosis. Additionally, the present invention relates to kits comprising the compound of the invention as well as to methods for devising said compound. Finally, the invention relates to methods for devising lead compounds for the development of the compounds of the invention.

机译：本发明涉及与正常或突变的GTP结合蛋白的表面结合并通过将至少一个官能团引入所述蛋白的活性位点来降低其GTP酶活性的活化能的化合物。所述化合物是合成或半合成来源的。优选地，上述官能团是精氨酸指或其衍生物或模拟例如通过拟肽获得的精氨酸指活性的化合物。本发明还涉及包含本发明化合物的药物组合物，以及治疗患有Ras基因致癌激活，G蛋白功能异常引起的肿瘤或神经纤维瘤病的患者的方法。另外，本发明涉及包含本发明化合物的试剂盒以及设计所述化合物的方法。最后，本发明涉及设计用于开发本发明化合物的先导化合物的方法。

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公开/公告号WO9902557A1

专利类型
公开/公告日1999-01-21

原文格式PDF
申请/专利权人 MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WISSENSCHAFTEN E.V;SCHEFFZEK KLAUS;AHMADIAN MOHAMMAD REZA;WITTINGHOFER ALFRED;
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申请/专利号WO1997EP03701
发明设计人 SCHEFFZEK KLAUS;AHMADIAN MOHAMMAD REZA;WITTINGHOFER ALFRED;
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申请日1997-07-11
分类号C07K14/47;
国家 WO
入库时间 2022-08-22 02:21:53

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