METHODS AND COMPOSITIONS FOR DETERMINING ISOMERASE ENZYMATIC ACTIVITY
    2.
    发明申请
    METHODS AND COMPOSITIONS FOR DETERMINING ISOMERASE ENZYMATIC ACTIVITY 失效
    用于测定异构酶酶活性的方法和组合物

    公开(公告)号:US20110020895A1

    公开(公告)日:2011-01-27

    申请号:US12875952

    申请日:2010-09-03

    IPC分类号: C12N9/96 C12N9/90 C07H21/04

    摘要: This disclosure provides crystalline flavonoid or flavanone isomerases, isolated non-native isomerase having the structural coordinates of said crystalline isomerase, and nucleic acids encoding such non-native isomerase. Also disclosed are methods of predicting the activity and/or substrate specificity of a putative isomerase, methods of identifying potential ismerase substrates, and methods of identifying potential isomerase inhibitors.

    摘要翻译: 本公开提供结晶类黄酮或黄烷酮异构酶,具有所述结晶异构酶的结构坐标的分离的非天然异构酶和编码这种非天然异构酶的核酸。 还公开了预测推定异构酶的活性和/或底物特异性的方法,鉴定潜在的ismerase底物的方法以及鉴定潜在的异构酶抑制剂的方法。

    Method of screening inhibitors of mevalonate-independent isoprenoid biosynthetic pathway
    10.
    发明授权
    Method of screening inhibitors of mevalonate-independent isoprenoid biosynthetic pathway 有权
    筛选甲羟戊酸依赖型异戊二烯生物合成途径抑制剂的方法

    公开(公告)号:US07286973B1

    公开(公告)日:2007-10-23

    申请号:US10240636

    申请日:2001-05-03

    IPC分类号: G06G7/58 C12N9/00

    摘要: The present invention provides the structure of the enzyme 4-diphosphocytidyl-2-C-methylerythritol (CDP-ME) synthase, a member of the cytidyltransferase family of enzymes from Escherichia coli. CDP-ME is a critical intermediate in the mevalonate-independent pathway for isoprenoid biosynthesis in a number of prokaryotic organisms, in algae, in the plastids of plants, and in the malaria parasite. Since vertebrates synthesize isoprenoid precursors using a mevalonate pathway, CDP-ME synthase and other enzymes of the mevalonate-independent pathway for isoprenoid production represent attractive targets for the structure-based design of selective antibacterial, herbicidal, and antimalarial drugs. Accordingly, the present invention provides methods for screening for compounds that inhibit enzymes of the mevalonate-independent pathway and pharmaceutical compositions and antibacterial formulations thereof. Further provided are methods of inhibiting the enzymes of the pathway and bacterial terpenoid synthesis and methods for treating a subject suffering from a bacterial infection.

    摘要翻译: 本发明提供了来自大肠杆菌的酶的β-二磷酸胞苷基-2-C-甲基赤藓糖醇(CDP-ME)合酶的细胞质转移酶家族的成员的结构。 CDP-ME是许多原核生物,藻类,植物质体和疟疾寄生虫中异戊二烯生物合成中甲羟甲酸非依赖途径的关键中间体。 由于脊椎动物使用甲羟戊酸途径合成类异戊二烯前体,所以CDP-ME合酶和甲醛酸非依赖性途径用于类异戊二烯生产的其它酶代表了选择性抗菌,除草和抗疟药物基于结构的设计的有吸引力的目标。 因此,本发明提供了筛选抑制甲羟戊酸依赖性途径的酶的化合物的方法及其药物组合物及其抗菌制剂。 还提供了抑制途径的酶和细菌萜类化合物合成的方法以及治疗患有细菌感染的受试者的方法。