Polyene polyketides, processes for their production and their use as a pharmaceutical
    1.
    发明授权
    Polyene polyketides, processes for their production and their use as a pharmaceutical 失效
    聚烯烃聚合物,其生产方法及其作为药物的用途

    公开(公告)号:US07416868B2

    公开(公告)日:2008-08-26

    申请号:US10760494

    申请日:2004-01-21

    IPC分类号: C12N9/00

    摘要: This invention relates to a new class of polyene polyketides, their pharmaceutically acceptable salts and derivatives, and to methods for obtaining the compounds. One method of obtaining these compounds is by cultivation of novel strains of Streptomyces aizunensis; another method involves expression of biosynthetic pathway genes in transformed host cells. The present invention further relates to the novel strains of Streptomyces aizunensis used to produce these compounds, to the use of these compounds and their pharmaceutically acceptable salts and derivatives as pharmaceuticals, in particular to their use as inhibitors of fungal cell growth and cancer cell growth. The invention also relates to pharmaceutical compositions comprising these novel polyketides or a pharmaceutically acceptable salts or derivatives thereof. Finally, the invention relates to novel polynucleotide sequences and their encoded proteins, which are involved in the biosynthesis of these novel polyketides.

    摘要翻译: 本发明涉及新类型的多烯聚酮化合物,其药学上可接受的盐和衍生物,以及获得化合物的方法。 获得这些化合物的一种方法是通过培养新的链霉菌链霉菌菌株; 另一种方法涉及在转化的宿主细胞中表达生物合成途径基因。 本发明还涉及用于制备这些化合物的新型链霉菌Streptomyces aizunensis菌株,使用这些化合物及其药学上可接受的盐和衍生物作为药物,特别是其作为真菌细胞生长抑制剂和癌细胞生长的用途。 本发明还涉及包含这些新型聚酮化合物或其药学上可接受的盐或衍生物的药物组合物。 最后,本发明涉及参与这些新型聚酮化合物的生物合成的新型多核苷酸序列及其编码的蛋白质。

    HIGH THROUGHPUT METHOD FOR DISCOVERY OF GENE CLUSTERS
    2.
    发明申请
    HIGH THROUGHPUT METHOD FOR DISCOVERY OF GENE CLUSTERS 审中-公开
    用于发现基因簇的高通量方法

    公开(公告)号:US20100016170A1

    公开(公告)日:2010-01-21

    申请号:US11803406

    申请日:2007-05-14

    IPC分类号: C40B20/04

    摘要: A method for identifying gene cluster is disclosed. The method may be used for identifying gene clusters involved in the biosynthesis of natural products. A small insert library of DNA fragments of genomic DNA and a large insert library of DNA fragments of genomic DNA are prepared. Fragments in the small insert library are sequenced and compared by homology comparison under computer control to a database containing genes, gene fragments or proteins known to be involved in the biosynthesis of microbial natural products. Fragments having similar structure to genes, gene fragments or proteins known to be involved in the biosynthesis of naturally occurring metabolites are used as probes to screen the large insert library of genomic DNA to detect gene clusters involved in the biosynthesis of microbial natural products.

    摘要翻译: 公开了鉴定基因簇的方法。 该方法可用于鉴定涉及天然产物生物合成的基因簇。 制备基因组DNA的DNA片段的小插入文库和基因组DNA的DNA片段的大插入文库。 对小插入片段中的片段进行测序,并通过计算机控制下的同源性比较与包含已知参与微生物天然产物生物合成的基因,基因片段或蛋白质的数据库进行比较。 具有与基因相似结构的片段,已知参与天然存在的代谢物的生物合成的基因片段或蛋白质被用作筛选基因组DNA的大插入文库以探测参与微生物天然产物生物合成的基因簇的片段。

    System, knowledge repository and computer-readable medium for identifying a secondary metabolite from a microorganism
    7.
    发明申请
    System, knowledge repository and computer-readable medium for identifying a secondary metabolite from a microorganism 审中-公开
    用于从微生物鉴定次级代谢物的系统,知识库和计算机可读介质

    公开(公告)号:US20080010025A1

    公开(公告)日:2008-01-10

    申请号:US11551137

    申请日:2006-10-19

    IPC分类号: G01N33/50

    CPC分类号: C12Q1/025

    摘要: The invention relates to a method and system for identifying a secondary metabolite synthesized by a target gene cluster within a microorganism. A putative or confirmed function is attributed to a gene within the gene cluster, and an extract from the microorganism is obtained which is suspected to contain the secondary metabolite synthesized by the gene cluster. The extract is then assessed for chemical, physical or biological properties, and the metabolite is identified and optionally isolated. Further, the invention provides a knowledge repository in which gene cluster information is linked to secondary metabolite production data. The invention further relates to a graphical user interface for accessing the knowledge repository, and a memory for storing data, having a data structure that is stored in the memory.

    摘要翻译: 本发明涉及鉴定由微生物内的靶基因簇合成的次级代谢物的方法和系统。 推定或确认的功能归因于基因簇内的基因,并且获得了怀疑含有由基因簇合成的次级代谢物的微生物提取物。 然后评估提取物的化学,物理或生物学性质,并鉴定和任选分离代谢物。 此外,本发明提供了知识库,其中基因簇信息与次级代谢产生数据相关联。 本发明还涉及用于访问知识库的图形用户界面和用于存储数据的存储器,其具有存储在存储器中的数据结构。

    Cyclic hexadepsipeptides, processes for their production and their use as pharmaceuticals
    8.
    发明授权
    Cyclic hexadepsipeptides, processes for their production and their use as pharmaceuticals 失效
    环十六肽,其制备方法及其作为药物的用途

    公开(公告)号:US08076287B2

    公开(公告)日:2011-12-13

    申请号:US12294213

    申请日:2007-03-28

    IPC分类号: A61K38/12

    摘要: The present invention provides cyclic hexadepsipeptides and their pharmaceutically acceptable salts, solvates and prodrugs, and methods for obtaining the compounds, by fermentation, optionally followed by post-biosynthesis chemical modification. The present invention further provides uses of cyclic hexadepsipeptides, and their pharmaceutically acceptable salts, solvates and prodrugs as pharmaceuticals, in particular to their use as antibacterial, antifungal or antineoplastic agents, and to pharmaceutical compositions comprising a cyclic hexadepsipeptide, or a pharmaceutically acceptable salt, solvate or prodrug thereof, together with a carrier.

    摘要翻译: 本发明提供环状十六肽及其药学上可接受的盐,溶剂合物和前药,以及通过发酵,任选地随后进行生物合成化学修饰来获得化合物的方法。 本发明进一步提供了环状十六肽及其药学上可接受的盐,溶剂合物和前药作为药物,特别是其作为抗细菌剂,抗真菌剂或抗肿瘤剂的用途的用途,以及包含环十六肽或其药学上可接受的盐, 溶剂化物或前药,以及载体。

    FARNESYL DIBENZODIAZEPINONE AND PROCESSES FOR ITS PRODUCTION
    9.
    发明申请
    FARNESYL DIBENZODIAZEPINONE AND PROCESSES FOR ITS PRODUCTION 审中-公开
    呋喃唑酮及其生产方法

    公开(公告)号:US20090263886A1

    公开(公告)日:2009-10-22

    申请号:US12400509

    申请日:2009-03-09

    IPC分类号: C12N1/21 C12N15/63 C07H21/04

    摘要: This invention relates to a novel farnesylated dibenzodiazepinone, named ECO-04601, its pharmaceutically acceptable salts and derivatives, and to methods for obtaining such compounds. One method of obtaining the ECO-04601 compound is by cultivation of a novel strain of Micromonospora sp., 046-ECO11; another method involves expression of biosynthetic pathway genes in transformed host cells. The present invention further relates to Micromonospora sp. strain 046-ECO11, to the use of and its pharmaceutically acceptable salts and derivatives as pharmaceuticals, in particular to their use as inhibitors of cancer cell growth, bacterial cell growth, mammalian lipoxygenase, and to pharmaceutical compositions comprising ECO-04601 or a pharmaceutically acceptable salt or derivative thereof. Finally, the invention relates to novel polynucleotide sequences and their encoded proteins, which are involved in the biosynthesis of ECO-04601.

    摘要翻译: 本发明涉及名为ECO-04601的新型法呢基化二苯并二氮杂酮,其药学上可接受的盐和衍生物,以及获得这些化合物的方法。 获得ECO-04601化合物的一种方法是通过培养一种新型的小单孢菌属菌株046-ECO11; 另一种方法涉及在转化的宿主细胞中表达生物合成途径基因。 本发明还涉及小单孢菌属 菌株046-ECO11,其药学上可接受的盐和衍生物用作药物,特别是其作为癌细胞生长抑制剂,细菌细胞生长,哺乳动物脂氧合酶的用途,以及包含ECO-04601或其药学上可接受的 盐或其衍生物。 最后,本发明涉及参与ECO-04601的生物合成的新型多核苷酸序列及其编码的蛋白质。