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    • 7. 发明授权
    • Crystals, molecular complexes, and methods of developing lead compounds for inhibitors of bacterial IMPDH
    • 晶体,分子复合物,以及开发用于细菌IMPDH抑制剂的铅化合物的方法
    • US06826488B1
    • 2004-11-30
    • US09533466
    • 2000-03-23
    • Frank R. CollartEliezer HubermanAndrezej JoachimiakRongguang ZhangEdwin M. Westbrook
    • Frank R. CollartEliezer HubermanAndrezej JoachimiakRongguang ZhangEdwin M. Westbrook
    • G06F1900
    • C12N9/0006C07K2299/00C12Y101/01205
    • The present invention relates to a data storage medium encoded with the structural coordinates of crystallized molecules and molecular complexes which comprise the active site binding pockets of bacterial IMPDH. Such data storage material is capable of displaying such molecules and molecular complexes, or their structural homologues, as a graphical three-dimensional representation on a computer screen. This invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention relates to methods of using the structure coordinates to screen and design compounds, including inhibitory compounds, that bind to IMPDH or homologues thereof. This invention also relates to molecules and molecular complexes that comprise the active site binding pockets of IMPDH or close structural homologues of the active site binding pockets. This invention also relates to compounds and pharmaceutical compositions which are inhibitors of bacterial IMPDH.
    • 本发明涉及用结构化分子和分子复合物的结构坐标编码的数据存储介质,其包含细菌IMPDH的活性位点结合口袋。 这样的数据存储材料能够在计算机屏幕上显示这样的分子和分子复合物或其结构同系物作为图形三维表示。 本发明还涉及使用结构坐标来解决同源蛋白质或蛋白质复合物的结构的方法。 此外,本发明涉及使用结构坐标来筛选和设计结合IMPDH或其同系物的化合物(包括抑制性化合物)的方法。 本发明还涉及包含IMPDH的活性位点结合袋或活性位点结合口袋的紧密结构同系物的分子和分子复合物。 本发明还涉及作为细菌IMPDH抑制剂的化合物和药物组合物。
    • 10. 发明授权
    • Methods and materials relating to IMPDH and GMP production
    • 与IMPDH和GMP生产有关的方法和材料
    • US06479628B1
    • 2002-11-12
    • US09712372
    • 2000-11-13
    • Frank R. CollartEliezer Huberman
    • Frank R. CollartEliezer Huberman
    • A61K3800
    • C12N9/0006A61K48/00C07K16/40C12P19/32C12Y101/01205
    • Disclosed are purified and isolated DNA sequences encoding eukaryotic proteins possessing biological properties of inosine 5′-monophosphate dehydrogenase (“IMPDH”). Illustratively, mammalian (e.g., human) IMPDH-encoding DNA sequences are useful in transformation or transfection of host cells for the large scale recombinant production of the enzymatically active expression products and/or products (e.g., GMP) resulting from IMPDH catalyzed synthesis in cells. Vectors including IMPDH-encoding DNA sequences are useful in gene amplification procedures. Recombinant proteins and synthetic peptides provided by the invention are useful as immunological reagents and in the preparation of antibodies (including polyclonal and monoclonal antibodies) for quantitative detection of IMPDH.
    • 公开了编码具有肌苷5'-单磷酸脱氢酶(“IMPDH”)的生物学性质的真核蛋白质的纯化和分离的DNA序列。 说明性地,哺乳动物(例如,人)IMPDH编码DNA序列可用于宿主细胞的转化或转染,用于大规模重组产生由细胞内的IMPDH催化合成产生的酶活性表达产物和/或产物(例如,GMP) 。 包含IMPDH编码DNA序列的载体可用于基因扩增过程。 本发明提供的重组蛋白质和合成肽可用作免疫学试剂和用于定量检测IMPDH的抗体(包括多克隆和单克隆抗体)的制备。