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1. 发明申请

WO2005093036A3 INHIBITORS OF SIDEROPHORE BIOSYNTHESIS IN FUNGI 审中-公开
标题翻译：真菌生物化学的抑制剂
公开(公告)号：WO2005093036A3
公开(公告)日：2006-06-08
申请号：PCT/EP2005002654
申请日：2005-03-11
申请人： AUSTRIA WIRTSCHAFTSSERVICE GMBH , HAAS HUBERTUS , SCHRETTL MARKUS
发明人： HAAS HUBERTUS , SCHRETTL MARKUS
IPC分类号： C12Q1/02 , A61K45/00 , A61P31/10 , C12G1/00 , C12N9/00 , C12N9/02 , C12N9/10 , C12N9/88 , C12N15/52 , C12Q1/18 , C12Q1/25 , C12Q1/68
CPC分类号： C12N9/88 , C12N9/0069 , C12N9/1029 , C12N9/93 , C12N15/52 , C12Q1/18
摘要： The present invention relates to methods for screening inhibitors of siderophore biosynthesis in fungi, preferably in Aspergillus species, particularly preferred in Aspergillus fumigatus comprising (a) contacting a cell expressing a fungal siderophore with a compound to be tested; (b) determining whether said cell is capable of siderophore biosynthesis in the presence of said compound to be tested when compared to a cell not contacted with said compound; and (c) identifying the compound which inhibits fungal siderophore biosynthesis. Accordingly, the invention also provides for a method for screening inhibitors of fungal siderophore biosynthesis comprising the steps of (a) contacting an enzyme involved in siderophore biosynthesis with a compound to be tested; (b) determining whether said enzyme is functional in the pathway of siderophore biosynthesis in the presence of said compounds to be tested when compared to an enzyme not contacted with said compound; and (c) identifying the compound which inhibits the enzymatic function involved in siderophore biosynthesis. In another aspect the present invention relates to a method of preparing a pharmaceutical composition for treating diseases associated with fungal infections, particularly, aspergillosis or coccidiosis comprising (a) identifying a compound which inhibits fungal sideropore biosynthesis; and (b) formulating said compound with a pharmaceutically acceptable carrier. In a further aspect, the present invention relates to a method for the production of a pharmaceutical composition comprising the steps of the aforementioned screening method and the subsequent step of mixing the compound identified to be an inhibitor of fungal siderophore biosynthesis with a pharmaceutically acceptable carrier. Moreover, the present invention envisages a pharmaceutical composition comprising an inhibitor of fungal siderophore biosynthesis as well as the use of such an inhibitor for the preparation of a pharmaceutical composition for the prevention and/or treatment of diseases associated with fungal infections, particularly, aspergillosis or coccidiosis.
摘要翻译：本发明涉及用于筛选真菌中铁载体生物合成抑制剂的方法，优选在曲霉菌种中，特别优选烟曲霉（Aspergillus fumigatus），其包括（a）使表达真菌载体的细胞与待测化合物接触; （b）当与未与所述化合物接触的细胞相比时，确定所述细胞是否能够在待测试化合物存在下进行铁载体生物合成; 和（c）鉴定抑制真菌铁载体生物合成的化合物。因此，本发明还提供了一种筛选真菌铁载体生物合成抑制剂的方法，包括以下步骤：（a）使参与铁载体生物合成的酶与待测化合物接触; （b）当与未与所述化合物接触的酶进行比较时，确定在所述待测化合物存在下，所述酶是否在铁载体生物合成途径中起作用; 和（c）鉴定抑制铁载体生物合成中涉及的酶功能的化合物。另一方面，本发明涉及制备用于治疗与真菌感染，特别是曲霉病或球虫病有关的疾病的药物组合物的方法，其包括（a）鉴定抑制真菌铁载体生物合成的化合物; 和（b）用药学上可接受的载体配制所述化合物。另一方面，本发明涉及制备药物组合物的方法，其包括上述筛选方法和随后的将被鉴定为真菌载体载体生物合成抑制剂的化合物与药学上可接受的载体混合的步骤。此外，本发明设想了包含真菌铁载体生物合成抑制剂的药物组合物以及这种抑制剂用于制备药物组合物用于预防和/或治疗与真菌感染相关的疾病，特别是曲霉病或球虫病。

2. 发明申请

WO2010032230A9 NON-AUXOTROPHIC SELECTION MARKER 审中-公开
公开(公告)号：WO2010032230A9
公开(公告)日：2010-03-25
申请号：PCT/IE2008/000091
申请日：2008-09-22
申请人： NATIONAL UNIVERSITY OF IRELAND, MAYNOOTH , CARBERRY, Stephen , DOYLE, John, Martin , HAAS, Hubertus , KAVANAGH, Kevin , SCHRETTL, Markus
发明人： CARBERRY, Stephen , DOYLE, John, Martin , HAAS, Hubertus , KAVANAGH, Kevin , SCHRETTL, Markus
IPC分类号： C12N15/65 , C12N1/14
摘要： A non-auxotrophic selection marker located in a gene cluster encoding a metabolite for an organism, such as a fungus, lacking said marker is provided. The selection marker gene can be used to detect and confirm the introduction of foreign genes without the use of exogenous drug-resistant genes to facilitate transformant selection. The selection marker gene can be applied to detect the presence of fungal infection and predict the likelihood of the development of disease or allergic response at an early stage so that medical intervention may be sought.

3. 发明申请

WO2005093036A2 INHIBITORS OF SIDEROPHORE BIOSYNTHESIS IN FUNGI 审中-公开
标题翻译：真菌生物化学抑制剂
公开(公告)号：WO2005093036A2
公开(公告)日：2005-10-06
申请号：PCT/EP2005/002654
申请日：2005-03-11
申请人： AUSTRIA WIRTSCHAFTSSERVICE GESELLSCHAFT MBH , HAAS, Hubertus , SCHRETTL, Markus
发明人： HAAS, Hubertus , SCHRETTL, Markus
IPC分类号： C12G1/00
CPC分类号： C12N9/88 , C12N9/0069 , C12N9/1029 , C12N9/93 , C12N15/52 , C12Q1/18
摘要： The present invention relates to methods for screening inhibitors of siderophore biosynthesis in fungi, preferably in Aspergillus species, particularly preferred in Aspergillus fumigatus comprising (a) contacting a cell expressing a fungal siderophore with a compound to be tested; (b) determining whether said cell is capable of siderophore biosynthesis in the presence of said compound to be tested when compared to a cell not contacted with said compound; and (c) identifying the compound which inhibits fungal siderophore biosynthesis. Accordingly, the invention also provides for a method for screening inhibitors of fungal siderophore biosynthesis comprising the steps of (a) contacting an enzyme involved in siderophore biosynthesis with a compound to be tested; (b) determining whether said enzyme is functional in the pathway of siderophore biosynthesis in the presence of said compounds to be tested when compared to an enzyme not contacted with said compound; and (c) identifying the compound which inhibits the enzymatic function involved in siderophore biosynthesis. In another aspect the present invention relates to a method of preparing a pharmaceutical composition for treating diseases associated with fungal infections, particularly, aspergillosis or coccidiosis comprising (a) identifying a compound which inhibits fungal sideropore biosynthesis; and (b) formulating said compound with a pharmaceutically acceptable carrier. In a further aspect, the present invention relates to a method for the production of a pharmaceutical composition comprising the steps of the aforementioned screening method and the subsequent step of mixing the compound identified to be an inhibitor of fungal siderophore biosynthesis with a pharmaceutically acceptable carrier. Moreover, the present invention envisages a pharmaceutical composition comprising an inhibitor of fungal siderophore biosynthesis as well as the use of such an inhibitor for the preparation of a pharmaceutical composition for the prevention and/or treatment of diseases associated with fungal infections, particularly, aspergillosis or coccidiosis.
摘要翻译：本发明涉及用于筛选真菌中铁载体生物合成抑制剂的方法，优选在曲霉菌种中，特别优选烟曲霉（Aspergillus fumigatus），其包括（a）使表达真菌载体的细胞与待测化合物接触; （b）当与未与所述化合物接触的细胞进行比较时，确定所述细胞是否能够在待测试化合物存在下进行铁载体生物合成; 和（c）鉴定抑制真菌铁载体生物合成的化合物。因此，本发明还提供了一种筛选真菌铁载体生物合成抑制剂的方法，包括以下步骤：（a）使参与铁载体生物合成的酶与待测化合物接触; （b）当与未与所述化合物接触的酶相比时，在所述待测化合物存在下，确定所述酶是否在铁载体生物合成途径中起作用; 和（c）鉴定抑制铁载体生物合成中涉及的酶功能的化合物。另一方面，本发明涉及制备用于治疗与真菌感染，特别是曲霉病或球虫病有关的疾病的药物组合物的方法，其包括（a）鉴定抑制真菌铁载体生物合成的化合物; 和（b）用药学上可接受的载体配制所述化合物。另一方面，本发明涉及制备药物组合物的方法，其包括上述筛选方法和随后的将被鉴定为真菌载体载体生物合成抑制剂的化合物与药学上可接受的载体混合的步骤。此外，本发明设想了包含真菌铁载体生物合成抑制剂的药物组合物以及这种抑制剂用于制备药物组合物用于预防和/或治疗与真菌感染相关的疾病，特别是曲霉病或球虫病。

4. 发明申请

WO2010032230A1 NON-AUXOTROPHIC SELECTION MARKER 审中-公开
标题翻译：非独立选择标记
公开(公告)号：WO2010032230A1
公开(公告)日：2010-03-25
申请号：PCT/IE2008000091
申请日：2008-09-22
申请人： NAT UNIV IRELAND MAYNOOTH , CARBERRY STEPHEN , DOYLE JOHN MARTIN , HAAS HUBERTUS , KAVANAGH KEVIN , SCHRETTL MARKUS
发明人： CARBERRY STEPHEN , DOYLE JOHN MARTIN , HAAS HUBERTUS , KAVANAGH KEVIN , SCHRETTL MARKUS
IPC分类号： C12N15/65 , C12N1/14
CPC分类号： C12N15/65 , C12N9/0036 , C12Y108/01009
摘要： A non-auxotrophic selection marker located in a gene cluster encoding a metabolite for an organism, such as a fungus, lacking said marker is provided. The selection marker gene can be used to detect and confirm the introduction of foreign genes without the use of exogenous drug-resistant genes to facilitate transformant selection. The selection marker gene can be applied to detect the presence of fungal infection and predict the likelihood of the development of disease or allergic response at an early stage so that medical intervention may be sought.
摘要翻译：提供了位于编码生物体代谢物的基因簇中的非营养缺陷型选择标记，例如缺乏所述标记的真菌。选择标记基因可用于检测和确认引入外源基因而不使用外源耐药基因以促进转化体选择。选择标记基因可用于检测真菌感染的存在，并预测早期发展疾病或过敏反应的可能性，以便寻求医疗干预。

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