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1.发明授权Methods of screening for compounds that inhibit the biosynthesis of GPI in malaria parasites 失效筛选疟原虫抑制GPI生物合成的化合物的方法公开(公告)号：US08252294B2
公开(公告)日：2012-08-28
申请号：US13040970
申请日：2011-03-04
申请人： Katsura Hata , Kaoru Ogawa , Itaru Tsukada , Kazutaka Nakamoto , Koji Sagane , Keigo Tanaka , Kappei Tsukahara , Toshihiro Horii
发明人： Katsura Hata , Kaoru Ogawa , Itaru Tsukada , Kazutaka Nakamoto , Koji Sagane , Keigo Tanaka , Kappei Tsukahara , Toshihiro Horii
IPC分类号： A61A39/015 , C07K12/00 , C07H21/04
CPC分类号： G01N33/573 , C07K14/445 , C12N9/1029 , C12Q1/18 , C12Q1/48 , G01N2333/37 , G01N2333/445 , G01N2500/04 , G01N2500/10
摘要： The present inventors succeeded in isolating GWT1 (PfGWT1), which is one of the enzymes involved in GPI biosynthesis in the malaria parasite P. falciparum. In addition, the inventors revealed that degenerate mutant DNAs, with a lower AT content than the DNA encoding the PfGWT1 protein, can complement the phenotype of GWT1-deficient yeast. Based on the findings, the present invention provides the GWT1 protein of malaria parasites and the use of the protein in methods of screening for antimalarial drugs. The present invention also provides degenerate mutant DNAs encoding proteins involved in GPI biosynthesis, and which have a lower AT content than the original DNAs. The present invention also provides methods of screening for antimalarial drugs which use the degenerate mutant DNAs.
摘要翻译： 本发明人成功地分离了在疟原虫恶性疟原虫中参与GPI生物合成的酶之一的GWT1（PfGWT1）。 此外，本发明人发现，与编码PfGWT1蛋白的DNA相比，AT含量低的退化突变体DNA可以补充GWT1缺陷型酵母的表型。 基于这些发现，本发明提供了疟疾寄生虫的GWT1蛋白和该蛋白在筛选抗疟疾药物的方法中的应用。 本发明还提供了编码参与GPI生物合成的蛋白质的简并突变DNA，其具有比原始DNA低的AT含量。 本发明还提供筛选使用简并突变DNA的抗疟疾药物的方法。
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公开(公告)号：US20090227799A1
公开(公告)日：2009-09-10
申请号：US11658901
申请日：2005-08-08
申请人： Kazutaka Nakamoto , Masayuki Matsukura , Keigo Tanaka , Satoshi Inoue , Itaru Tsukada , Toru Haneda , Norihiro Ueda , Shinya Abe , Koji Sagane
发明人： Kazutaka Nakamoto , Masayuki Matsukura , Keigo Tanaka , Satoshi Inoue , Itaru Tsukada , Toru Haneda , Norihiro Ueda , Shinya Abe , Koji Sagane
IPC分类号： C07D409/12
CPC分类号： C07D405/12 , C07D409/12
摘要： Disclosed is an antimalarial agent containing a compound represented by the formula: [wherein A1 represents a 3-pyridyl group that may have a substituent, a 6-quinolyl group that may have a substituent, or the like; X1 represents a group represented by the formula —C(═O)—NH— or the like; E represents a furyl group, a thienyl group or a phenyl group; with the proviso that A1 may have one to three substituents, and E has one of two substituents] or a salt thereof or hydrates thereof.
摘要翻译： 公开了含有下式表示的化合物的抗疟剂：[式中，A1表示可具有取代基的3-吡啶基，可具有取代基的6-喹啉基等。 X1表示由式-C（ - ）-NH-等表示的基团; E表示呋喃基，噻吩基或苯基; 条件是A1可以具有一至三个取代基，并且E具有两个取代基之一]或其盐或其水合物。
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公开(公告)号：US20090098636A1
公开(公告)日：2009-04-16
申请号：US12103609
申请日：2008-04-15
申请人： Kappei Tsukahara , Katsura Hata , Koji Sagane , Kazutaka Nakamoto , Mamiko Tsuchiya , Naoaki Watanabe , Fuminori Ohba , Itaru Tsukada , Norihiro Ueda , Keigo Tanaka , Junko Kai
发明人： Kappei Tsukahara , Katsura Hata , Koji Sagane , Kazutaka Nakamoto , Mamiko Tsuchiya , Naoaki Watanabe , Fuminori Ohba , Itaru Tsukada , Norihiro Ueda , Keigo Tanaka , Junko Kai
IPC分类号： C12N1/19
CPC分类号： C07K14/40 , A61K31/00 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/44 , A61K31/472 , A61K31/4725 , A61K31/5377 , A61K38/00 , C07D213/68 , C07D217/18 , C07D217/20 , C07K14/37 , C07K14/38 , C07K14/39 , C07K14/395 , C07K2319/02 , G01N2500/00 , Y10S435/911
摘要： A reporter system reflecting the transport process that transports GPI-anchored proteins to the cell wall was constructed and compounds inhibiting this process were discovered. Further, genes conferring resistance to the above compounds were identified and methods of screening for compounds that inhibit the activity of the proteins encoded by these genes were developed. Therefore, through the novel compounds, the present invention showed that antifungal agents having a novel mechanism, i.e. inhibiting the process that transports GPI-anchored proteins to the cell wall, could be achieved.
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公开(公告)号：US20080166765A1
公开(公告)日：2008-07-10
申请号：US11958310
申请日：2007-12-17
申请人： Kappei Tsukahara , Katsura Hata , Koji Sagane , Kazutaka Nakamoto , Mamiko Tsuchiya , Naoaki Watanabe , Fuminori Oba , Itaru Tsukada , Norihiro Ueda , Keigo Tanaka , Junko Kai
发明人： Kappei Tsukahara , Katsura Hata , Koji Sagane , Kazutaka Nakamoto , Mamiko Tsuchiya , Naoaki Watanabe , Fuminori Oba , Itaru Tsukada , Norihiro Ueda , Keigo Tanaka , Junko Kai
CPC分类号： C07K14/40 , A61K31/00 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/44 , A61K31/472 , A61K31/4725 , A61K31/5377 , A61K38/00 , C07D213/68 , C07D217/18 , C07D217/20 , C07K14/37 , C07K14/38 , C07K14/39 , C07K14/395 , C07K2319/02 , G01N2500/00 , Y10S435/911
摘要： A reporter system reflecting the transport process that transports GPI-anchored proteins to the cell wall was constructed and compounds inhibiting this process were discovered. Further, fungal genes conferring resistance to the above compounds were identified and methods of screening for compounds that inhibit the activity of the proteins encoded by these genes were developed. These genes encode proteins participating in fungal cell wall synthesis. Therefore, through the novel compounds, the present invention showed that antifungal agents having a novel mechanism, i.e. inhibiting the process that transports GPI-anchored proteins to the cell wall, could be achieved.
摘要翻译： 构建了将GPI锚定蛋白转运至细胞壁的运输过程的记录系统，发现了抑制该过程的化合物。 此外，鉴定了赋予对上述化合物的抗性的真菌基因，并开发了筛选抑制由这些基因编码的蛋白质的活性的化合物的方法。 这些基因编码参与真菌细胞壁合成的蛋白质。 因此，通过本发明，可以实现具有新机理的抗真菌剂，即抑制将GPI锚定蛋白转运到细胞壁的过程。
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5.发明授权Methods of screening for compounds that inhibit the biosynthesis of GPI in malaria parasites 失效筛选疟原虫抑制GPI生物合成的化合物的方法公开(公告)号：US07928215B2
公开(公告)日：2011-04-19
申请号：US10535928
申请日：2003-11-21
申请人： Katsura Hata , Kaoru Ogawa , Itaru Tsukada , Kazutaka Nakamoto , Koji Sagane , Keigo Tanaka , Kappei Tsukahara , Toshihiro Horii
发明人： Katsura Hata , Kaoru Ogawa , Itaru Tsukada , Kazutaka Nakamoto , Koji Sagane , Keigo Tanaka , Kappei Tsukahara , Toshihiro Horii
CPC分类号： G01N33/573 , C07K14/445 , C12N9/1029 , C12Q1/18 , C12Q1/48 , G01N2333/37 , G01N2333/445 , G01N2500/04 , G01N2500/10
摘要： The present inventors succeeded in isolating GWT1 (PfGWT1), which is one of the enzymes involved in GPI biosynthesis in the malaria parasite P. falciparum. In addition, the inventors revealed that degenerate mutant DNAs, with a lower AT content than the DNA encoding the PfGWT1 protein, can complement the phenotype of GWT1-deficient yeast. Based on the findings, the present invention provides the GWT1 protein of malaria parasites and the use of the protein in methods of screening for antimalarial drugs. The present invention also provides degenerate mutant DNAs encoding proteins involved in GPI biosynthesis, and which have a lower AT content than the original DNAs. The present invention also provides methods of screening for antimalarial drugs which use the degenerate mutant DNAs.
摘要翻译： 本发明人成功地分离了在疟原虫恶性疟原虫中参与GPI生物合成的酶之一的GWT1（PfGWT1）。 此外，本发明人发现，与编码PfGWT1蛋白的DNA相比，AT含量低的退化突变体DNA可以补充GWT1缺陷型酵母的表型。 基于这些发现，本发明提供了疟疾寄生虫的GWT1蛋白和该蛋白在筛选抗疟疾药物的方法中的应用。 本发明还提供了编码参与GPI生物合成的蛋白质的简并突变DNA，其具有比原始DNA低的AT含量。 本发明还提供筛选使用简并突变DNA的抗疟疾药物的方法。
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公开(公告)号：US20100333216A1
公开(公告)日：2010-12-30
申请号：US11988619
申请日：2006-07-12
申请人： Koji Sagane , Eiki Takahashi , Kazuto Yamazaki , Turo Oki
发明人： Koji Sagane , Eiki Takahashi , Kazuto Yamazaki , Turo Oki
IPC分类号： G01N33/00 , A01K67/00 , A01K67/027 , C12N5/16 , C12N5/18 , C12N15/873 , A61K38/48 , C12N9/50 , C12N15/85 , A61K31/7088 , A61P25/00
CPC分类号： A01K67/0276 , A01K2217/075 , A01K2227/105 , A01K2267/0356 , A61K38/00 , C12N9/6489 , C12N15/8509 , G01N33/5088
摘要： It is an object of the present invention to provide a non-human gene-disrupted animal with a disrupted ADAM11 gene. According to the present invention, a non-human gene-disrupted animal, wherein either one of or both alleles of an ADAM11 gene are disrupted, is provided.
摘要翻译： 本发明的目的是提供具有破坏的ADAM11基因的非人基因破坏的动物。 根据本发明，提供了非人基因破坏的动物，其中ADAM11基因的一个或两个等位基因被破坏。
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7.发明申请METHOD FOR ASSAYING ACTION OF ANTITUMOR AGENT USING SPLICING DEFECTS AS INDEX 审中-公开使用分离缺陷作为指标测定抗菌剂的作用方法公开(公告)号：US20100021918A1
公开(公告)日：2010-01-28
申请号：US12529959
申请日：2008-03-05
申请人： Yoshiharu Mizui , Naoko Hata , Masao Iwata , Koji Sagane , Mai Uesugi , Tadashi Kadowaki , Taku Yoshida
发明人： Yoshiharu Mizui , Naoko Hata , Masao Iwata , Koji Sagane , Mai Uesugi , Tadashi Kadowaki , Taku Yoshida
CPC分类号： G01N33/5011 , C12Q1/6883 , G01N33/68
摘要： An object of the present invention is to provide a method, a probe, a primer, an antibody, a reagent, and a kit for assaying an action of a pladienolide derivative to a living subject. According to the present invention, there is provided a method for assaying an action of the pladienolide derivative using splicing defect as an index.
摘要翻译： 本发明的目的是提供一种方法，探针，引物，抗体，试剂和用于测定普遍二烯内酰脲衍生物对活体的作用的试剂盒。 根据本发明，提供了使用拼接缺陷作为指标来测定扁桃苷内酰胺衍生物的作用的方法。
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8.发明申请TARGET MOLECULES OF PLADIENOLIDES, COMPOUNDS BINDING TO SUCH TARGET MOLECULES, AND SCREENING METHOD THEREOF 审中-公开对这些目标分子的化合物，化合物的目标分子和筛选方法公开(公告)号：US20090227795A1
公开(公告)日：2009-09-10
申请号：US12375516
申请日：2007-08-02
申请人： Yoshihiko Kotake , Koji Sagane , Takashi Owa , Yoshiharu Mizui , Hajime Shimizu , Yuko Kiyosue
发明人： Yoshihiko Kotake , Koji Sagane , Takashi Owa , Yoshiharu Mizui , Hajime Shimizu , Yuko Kiyosue
IPC分类号： C07D405/14 , G01N33/566 , C07D409/14 , C07F5/02 , C07D407/06 , A61P35/00
CPC分类号： A61K31/365 , A61K31/496 , C07D407/04 , C07D495/04 , G01N33/6875 , G01N2500/04
摘要： A method of measuring the binding activity of a test compound to a splicing factor 3b (SF3b), which comprises the following steps of: (a) contacting a labeled pladienolide compound and a test compound with a cell or a cell fraction; and (b) measuring the distribution of the bound labeled compound. The method enables to screen for a novel active compound capable of acting on (binding to) a pladienolide target molecule or the like.
摘要翻译： 测试化合物与剪接因子3b（SF3b）的结合活性的方法，其包括以下步骤：（a）使标记的普拉二烯内酯化合物和测试化合物与细胞或细胞级分接触; 和（b）测量结合的标记化合物的分布。 该方法能够筛选能够作用于（结合）扁桃苷内酯靶分子等的新型活性化合物。
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公开(公告)号：US20060234283A1
公开(公告)日：2006-10-19
申请号：US11409453
申请日：2006-04-21
申请人： Kappei Tsukahara , Katsura Hata , Koji Sagane , Kazutaka Nakamoto , Mamiko Tsuchiya , Naoaki Watanabe , Fuminori Ohba , Itaru Tsukada , Norihiro Ueda , Keigo Tanaka , Junko Kai
发明人： Kappei Tsukahara , Katsura Hata , Koji Sagane , Kazutaka Nakamoto , Mamiko Tsuchiya , Naoaki Watanabe , Fuminori Ohba , Itaru Tsukada , Norihiro Ueda , Keigo Tanaka , Junko Kai
IPC分类号： C12Q1/68 , G01N33/569 , G01N33/53
CPC分类号： C07K14/40 , A61K31/00 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/44 , A61K31/472 , A61K31/4725 , A61K31/5377 , A61K38/00 , C07D213/68 , C07D217/18 , C07D217/20 , C07K14/37 , C07K14/38 , C07K14/39 , C07K14/395 , C07K2319/02 , G01N2500/00 , Y10S435/911
摘要： A reporter system reflecting the transport process that transports GPI-anchored proteins to the cell wall was constructed and compounds inhibiting this process were discovered. Further, genes conferring resistance to the above compounds were identified and methods of screening for compounds that inhibit the activity of the proteins encoded by these genes were developed. Therefore, through the novel compounds, the present invention showed that antifungal agents having a novel mechanism, i.e. inhibiting the process that transports GPI-anchored proteins to the cell wall, could be achieved.
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10.发明申请Methods of screening for compounds that inhibit the biosynthesis of gpi in malaria parasites 失效筛选抑制疟疾寄生虫中gpi生物合成的化合物的方法公开(公告)号：US20060172404A1
公开(公告)日：2006-08-03
申请号：US10535928
申请日：2003-11-21
申请人： Katsura Hata , Kaoru Ogawa , Itaru Tsukada , Kazutaka Nakamoto , Koji Sagane , Keigo Tanaka , Kappei Tsukahara , Toshihiro Horii
发明人： Katsura Hata , Kaoru Ogawa , Itaru Tsukada , Kazutaka Nakamoto , Koji Sagane , Keigo Tanaka , Kappei Tsukahara , Toshihiro Horii
CPC分类号： G01N33/573 , C07K14/445 , C12N9/1029 , C12Q1/18 , C12Q1/48 , G01N2333/37 , G01N2333/445 , G01N2500/04 , G01N2500/10
摘要： The present inventors succeeded in isolating GWT1 (PfGWT1), which is one of the enzymes involved in GPI biosynthesis in the malaria parasite P. falciparum. In addition, the inventors revealed that degenerate mutant DNAs, with a lower AT content than the DNA encoding the PfGWT1 protein, can complement the phenotype of GWT1-deficient yeast. Based on the findings, the present invention provides the GWT1 protein of malaria parasites and the use of the protein in methods of screening for antimalarial drugs. The present invention also provides degenerate mutant DNAs encoding proteins involved in GPI biosynthesis, and which have a lower AT content than the original DNAs. The present invention also provides methods of screening for antimalarial drugs which use the degenerate mutant DNAs.
摘要翻译： 本发明人成功地分离了在疟原虫恶性疟原虫中参与GPI生物合成的酶之一的GWT1（PfGWT1）。 此外，本发明人发现，具有比编码PfGWT1蛋白质的DNA低的AT含量的简并突变DNA可以补充GWT1缺陷型酵母的表型。 基于这些发现，本发明提供了疟疾寄生虫的GWT1蛋白和该蛋白在筛选抗疟疾药物的方法中的应用。 本发明还提供了编码参与GPI生物合成的蛋白质的简并突变DNA，其具有比原始DNA低的AT含量。 本发明还提供筛选使用简并突变DNA的抗疟疾药物的方法。
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