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1.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
CPC分类号： C12N9/1205 , C40B30/02 , G06F19/16 , G06F19/706 , Y02A90/26
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。
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2.发明申请METHODS OF PRODUCING POLYKETIDE SYNTHASE MUTANTS AND COMPOSITIONS AND USES THEREOF 审中-公开生产多肽合成酶突变体及其组合物的方法及其用途公开(公告)号：US20120096581A1
公开(公告)日：2012-04-19
申请号：US12897723
申请日：2010-10-04
CPC分类号： C12Y203/01074 , C07K2299/00 , C12N9/00 , C12N9/1037 , C12N15/52
摘要： The present invention comprises crystalline polyketide synthases, isolated non-native polyketide synthases having the structural coordinates of said crystalline polyketide synthases, and nucleic acid encoding such non-native polyketide synthases. Also disclosed are methods of producing mutant polyketide synthases, and methods of altering the activity and/or substrate specificity of putative polyketide synthases.
摘要翻译： 本发明包括结晶聚酮化合物合成酶，具有所述结晶聚酮化合物合酶的结构坐标的分离的非天然聚酮化合物合酶和编码这种非天然聚酮化合物合酶的核酸。 还公开了产生突变体聚酮化合物合酶的方法，以及改变推定的聚酮化合物合酶的活性和/或底物特异性的方法。
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3.发明申请METHODS OF PRODUCING POLYKETIDE SYNTHASE MUTANTS AND COMPOSITIONS AND USES THEREOF 有权生产多肽合成酶突变体及其组合物的方法及其用途公开(公告)号：US20090271888A1
公开(公告)日：2009-10-29
申请号：US11876767
申请日：2007-10-22
CPC分类号： C12Y203/01074 , C07K2299/00 , C12N9/00 , C12N9/1037 , C12N15/52
摘要： The present invention comprises crystalline polyketide synthases, isolated non-native polyketide synthases having the structural coordinates of said crystalline polyketide synthases, and nucleic acid encoding such non-native polyketide synthases. Also disclosed are methods of producing mutant polyketide synthases, and methods of altering the activity and/or substrate specificity of putative polyketide synthases.
摘要翻译： 本发明包括结晶聚酮化合物合成酶，具有所述结晶聚酮化合物合酶的结构坐标的分离的非天然聚酮化合物合酶和编码这种非天然聚酮化合物合酶的核酸。 还公开了产生突变体聚酮化合物合酶的方法，以及改变推定的聚酮化合物合酶的活性和/或底物特异性的方法。
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4.发明授权Methods of producing polyketide synthase mutants and compositions and uses thereof 有权生产聚酮化合物合酶突变体的方法及其组合物和用途公开(公告)号：US07285380B2
公开(公告)日：2007-10-23
申请号：US10450230
申请日：2001-12-14
CPC分类号： C12Y203/01074 , C07K2299/00 , C12N9/00 , C12N9/1037 , C12N15/52
摘要： The present invention comprises crystalline polyketide synthases, isolated non-native polyketide synthases having the structural coordinates of said crystalline polyketide synthases, and nucleic acids encoding such non-native polyketide synthases. Also disclosed are methods of producing mutant polyketide synthases, and methods of altering the activity and/or substrate specificity of putative polyketide synthases.
摘要翻译： 本发明包括结晶聚酮化合物合成酶，具有所述结晶聚酮化合物合酶的结构坐标的分离的非天然聚酮化合物合酶和编码这种非天然聚酮化合物合酶的核酸。 还公开了产生突变体聚酮化合物合酶的方法，以及改变推定的聚酮化合物合酶的活性和/或底物特异性的方法。
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5.发明申请INCORPORATION OF TYPE III POLYKETIDE SYNTHASES INTO MULTIDOMAIN PROTEINS OF THE TYPE I AND III POLYKETIDE SYNTHASE AND FATTY ACID SYNTHASE FAMILIES 审中-公开将III型聚合酶合成酶掺入I型和III型多肽合成酶和脂肪酸合成酶家族的多种蛋白质公开(公告)号：US20120122180A1
公开(公告)日：2012-05-17
申请号：US13294939
申请日：2011-11-11
IPC分类号： C12N9/96
CPC分类号： C12N15/52 , C07K2319/00
摘要： Recombinant fusion proteins in which intermediates are covalently bound to the fusion proteins and transferred between domains of the fusion proteins are provided. The fusion proteins include proteins having type I polyketide or fatty acid synthase domains fused with type III polyketide synthase domains. Methods of making such recombinant fusion proteins and methods using such proteins to produce polyketide and other products are described.
摘要翻译： 提供其中中间体与融合蛋白共价结合并在融合蛋白的结构域之间转移的重组融合蛋白。 融合蛋白包括与III型聚酮化合物结构域融合的具有I型聚酮化合物或脂肪酸合酶结构域的蛋白质。 描述了制备这种重组融合蛋白的方法和使用这种蛋白质产生聚酮化合物和其它产物的方法。
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6.发明授权Methods of producing polyketide synthase mutants and compositions and uses thereof 有权生产聚酮化合物合酶突变体的方法及其组合物和用途公开(公告)号：US07807424B2
公开(公告)日：2010-10-05
申请号：US11876767
申请日：2007-10-22
CPC分类号： C12Y203/01074 , C07K2299/00 , C12N9/00 , C12N9/1037 , C12N15/52
摘要： The present invention comprises crystalline polyketide synthases, isolated non-native polyketide synthases having the structural coordinates of said crystalline polyketide synthases, and nucleic acid encoding such non-native polyketide synthases. Also disclosed are methods of producing mutant polyketide synthases, and methods of altering the activity and/or substrate specificity of putative polyketide synthases.
摘要翻译： 本发明包括结晶聚酮化合物合成酶，具有所述结晶聚酮化合物合酶的结构坐标的分离的非天然聚酮化合物合酶和编码这种非天然聚酮化合物合酶的核酸。 还公开了产生突变体聚酮化合物合酶的方法，以及改变推定的聚酮化合物合酶的活性和/或底物特异性的方法。
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7.发明授权公开(公告)号：US07792645B2
公开(公告)日：2010-09-07
申请号：US10344051
申请日：2001-08-29
CPC分类号： C12N15/825 , A61K38/00 , C07K2299/00 , C12N9/90 , C12Y505/01006
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 isomerase 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，鉴定潜在的异构酶底物的方法以及鉴定潜在的异构酶抑制剂的方法。
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公开(公告)号：US20110020895A1
公开(公告)日：2011-01-27
申请号：US12875952
申请日：2010-09-03
CPC分类号： C12N15/825 , A61K38/00 , C07K2299/00 , C12N9/90 , C12Y505/01006
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。
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公开(公告)号：US20090011400A1
公开(公告)日：2009-01-08
申请号：US11998828
申请日：2007-11-30
IPC分类号： C12Q1/00 , C12N9/00 , C12N15/11 , C12N1/20 , C12N1/19 , C12N5/04 , C12N5/06 , C40B40/10 , G06G7/50
CPC分类号： C12N9/88
摘要： Crystal structure information is used to make substrate-switched amino acid ammonia lyase enzymes, including TALs, PALs and HALs. Related methods, systems, compositions, cells and transgenic organisms are provided.
摘要翻译： 晶体结构信息用于制备底物转换氨基酸氨裂解酶，包括TAL，PAL和HAL。 提供了相关方法，系统，组合物，细胞和转基因生物。
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10.发明申请Incorporation of type III polyketide synthases into multidomain proteins of the type I and III polyketide synthase and fatty acid synthase families 审中-公开将I型聚酮化合物合酶引入I型和III型聚酮化合物合酶和脂肪酸合酶家族的多结构域蛋白公开(公告)号：US20080233628A1
公开(公告)日：2008-09-25
申请号：US11901264
申请日：2007-09-13
CPC分类号： C12N15/52 , C07K2319/00
摘要： Recombinant fusion proteins in which intermediates are covalently bound to the fusion proteins and transferred between domains of the fusion proteins are provided. The fusion proteins include proteins having type I polyketide or fatty acid synthase domains fused with type III polyketide synthase domains. Methods of making such recombinant fusion proteins and methods using such proteins to produce polyketide and other products are described.
摘要翻译： 提供其中中间体与融合蛋白共价结合并在融合蛋白的结构域之间转移的重组融合蛋白。 融合蛋白包括与III型聚酮化合物结构域融合的具有I型聚酮化合物或脂肪酸合酶结构域的蛋白质。 描述了制备这种重组融合蛋白的方法和使用这种蛋白质产生聚酮化合物和其它产物的方法。
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