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公开(公告)号：US20110014216A1
公开(公告)日：2011-01-20
申请号：US12681450
申请日：2008-10-02
申请人： Andreas Brecht , Florent Beaufils
发明人： Andreas Brecht , Florent Beaufils
CPC分类号： C07H19/207 , A61K38/00 , A61K47/549 , A61K47/55 , A61K47/595 , A61K47/60 , A61K49/0002 , A61K49/0028 , A61K49/0043 , A61K49/0052 , A61K49/0054 , C07K14/245 , C12N15/62
摘要： The invention relates to coenzyme A (CoA) type compounds carrying one or more drug entities and optionally a label detectable by a fluorescence detector, magnetic resonance imaging (MRI), positron emission tomography (PET) or scintigraphy, and/or a functional group which can be transformed into a drug or a detectable label. The invention further relates to a molecular shuttle which is a fusion protein comprising a proteinaceous binding entity directed to a target and an acyl carrier protein (ACP) or a fragment thereof, and carrying one or more drug entities. The proteinaceous binding entity is designed to bind to a target structure in vitro or in vivo, for example a cellular receptor.
摘要翻译： 本发明涉及携带一种或多种药物实体的辅酶A（CoA）型化合物和任选的可由荧光检测器，磁共振成像（MRI），正电子发射断层摄影（PET）或闪烁扫描技术检测的标记物和/或官能团， 可以转化成药物或可检测标签。 本发明还涉及分子穿梭，其是包含靶向靶蛋白质结合实体和酰基载体蛋白（ACP）或其片段并携带一种或多种药物实体的融合蛋白。 蛋白质结合实体被设计为在体外或体内结合靶结构，例如细胞受体。
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公开(公告)号：US08227602B2
公开(公告)日：2012-07-24
申请号：US12309554
申请日：2007-07-24
IPC分类号： C07D239/02
CPC分类号： G01N33/581 , C07D239/47 , C07D403/14 , C07D405/12 , C07D487/04 , C12N9/12 , C12Q1/48
摘要： The invention relates to new proteins called alkylcytosine transferases (ACTs) derived from O6-alkylguanine-DNA alkyltransferase, and to substrates for ACTs specifically transferring a label to these ACTs and to fusion proteins comprising these. The substrates according of the invention are substituted cytosines of formula (I) wherein R1 is an aromatic or a heteroaromatic group, or an optionally substituted unsaturated alkyl, cycloalkyl or heterocyclyl group with the double bond connected to OCH2—; R2 is a linker; and L is a label or a plurality of same or different labels. The invention further relates to methods of transferring label L from these substrates of formula (I) to ACTs and ACT fusion proteins. The system of ACT-compound of formula (I) is particularly suitable for double labelling studies together with the known system O6-alkylguanine-DNA alkyltransferase (AGT)-benzylguanines.
摘要翻译： 本发明涉及从O6-烷基鸟嘌呤-DNA烷基转移酶衍生的称为烷基胞嘧啶转移酶（ACT）的新蛋白质，以及特异性将标记转移至这些ACT的ACT的底物和包含它们的融合蛋白。 根据本发明的底物是其中R 1是芳族或杂芳族基团的式（I）的取代的胞嘧啶或具有与OCH 2连接的双键的任选取代的不饱和烷基，环烷基或杂环基; R2是连接体; L是标签或多个相同或不同的标签。 本发明还涉及将标记L从这些式（I）底物转移到ACT和ACT融合蛋白的方法。 式（I）的ACT-化合物的系统特别适用于已知的系统O6-烷基鸟嘌呤-DNA烷基转移酶（AGT） - 苄基胍的双重标记研究。
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公开(公告)号：US20110207157A1
公开(公告)日：2011-08-25
申请号：US12309554
申请日：2007-07-24
IPC分类号： C12Q1/48 , C12N9/10 , C40B30/00 , C07D239/47 , C07D405/12 , C07D403/14 , C07D495/04 , C07D493/10 , C12N9/96
CPC分类号： G01N33/581 , C07D239/47 , C07D403/14 , C07D405/12 , C07D487/04 , C12N9/12 , C12Q1/48
摘要： The invention relates to new proteins called alkylcytosine transferases (ACTs) derived from O6-alkylguanine-DNA alkyltransferase, and to substrates for ACTs specifically transferring a label to these ACTs and to fusion proteins comprising these. The substrates according of the invention are substituted cytosines of formula (I) wherein R1 is an aromatic or a heteroaromatic group, or an optionally substituted unsaturated alkyl, cycloalkyl or heterocyclyl group with the double bond connected to OCH2—; R2 is a linker; and L is a label or a plurality of same or different labels. The invention further relates to methods of transferring label L from these substrates of formula (I) to ACTs and ACT fusion proteins. The system of ACT-compound of formula (I) is particularly suitable for double labelling studies together with the known system O6-alkylguanine-DNA alkyltransferase (AGT)-benzylguanines.
摘要翻译： 本发明涉及从O6-烷基鸟嘌呤-DNA烷基转移酶衍生的称为烷基胞嘧啶转移酶（ACT）的新蛋白质，以及将这些ACT特异性转移标记物的ACT和包含这些酶的融合蛋白质的底物。 根据本发明的底物是其中R 1是芳族或杂芳族基团的式（I）的取代的胞嘧啶或具有与OCH 2连接的双键的任选取代的不饱和烷基，环烷基或杂环基; R2是连接体; L是标签或多个相同或不同的标签。 本发明还涉及将标记L从这些式（I）底物转移到ACT和ACT融合蛋白的方法。 式（I）的ACT-化合物的系统特别适用于已知的系统O6-烷基鸟嘌呤-DNA烷基转移酶（AGT） - 苄基胍的双重标记研究。
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公开(公告)号：US20120237961A1
公开(公告)日：2012-09-20
申请号：US13484954
申请日：2012-05-31
CPC分类号： G01N33/581 , C07D239/47 , C07D403/14 , C07D405/12 , C07D487/04 , C12N9/12 , C12Q1/48
摘要： The invention relates to new proteins called alkylcytosine transferases (ACTs) derived from O6-alkylguanine-DNA alkyltransferase, and to substrates for ACTs specifically transferring a label to these ACTs and to fusion proteins comprising these. The substrates according of the invention are substituted cytosines of formula (I) wherein R1 is an aromatic or a heteroaromatic group, or an optionally substituted unsaturated alkyl, cycloalkyl or heterocyclyl group with the double bond connected to OCH2—; R2 is a linker; and L is a label or a plurality of same or different labels. The invention further relates to methods of transferring label L from these substrates of formula (I) to ACTs and ACT fusion proteins. The system of ACT-compound of formula (I) is particularly suitable for double labelling studies together with the known system O6-alkylguanine-DNA alkyltransferase (AGT)-benzylguanines.
摘要翻译： 本发明涉及从O6-烷基鸟嘌呤-DNA烷基转移酶衍生的称为烷基胞嘧啶转移酶（ACT）的新蛋白质，以及将这些ACT特异性转移标记物的ACT和包含这些酶的融合蛋白质的底物。 根据本发明的底物是其中R 1是芳族或杂芳族基团的式（I）的取代的胞嘧啶或具有与OCH 2连接的双键的任选取代的不饱和烷基，环烷基或杂环基; R2是连接体; L是标签或多个相同或不同的标签。 本发明还涉及将标记L从这些式（I）底物转移到ACT和ACT融合蛋白的方法。 式（I）的ACT-化合物的系统特别适用于已知的系统O6-烷基鸟嘌呤-DNA烷基转移酶（AGT） - 苄基胍的双重标记研究。
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公开(公告)号：US20110014196A1
公开(公告)日：2011-01-20
申请号：US12681442
申请日：2008-10-02
申请人： Andreas Brecht , Florent Beaufils
发明人： Andreas Brecht , Florent Beaufils
IPC分类号： A61K39/395 , C12N9/10 , A61P35/00 , C07D473/18 , C07H21/02 , C07H19/167 , A61K31/713 , A61K31/522 , A61K31/7076 , A61K31/538 , A61K38/45
CPC分类号： C07H19/167 , A61K47/545 , A61K47/556 , A61K47/64 , A61K47/67 , A61K49/0002 , A61K49/0026 , A61K49/0028 , A61K49/0039 , A61K49/0041 , A61K49/0043 , A61K49/0052 , A61K49/0054 , B82Y5/00 , C07D473/18
摘要： The invention relates to compounds comprising a plurality of enzyme substrates suitably linked and further carrying one or more cargo entities. In particular such compounds have the structure (substrate)n-linker-(cargo)m wherein “substrate” is a substrate specific for an enzyme-type protein; n is 2 or more; “linker” is a linking unit consisting of 1 to 300 atoms; “cargo” is a drug, a label detectable by a fluorescence detector, magnetic resonance imaging (MRI), positron emission tomography (PET) or scintigraphy, or a functional group which can be transformed into a drug or a detectable label; and m is 1 or more. The invention further relates to a corresponding molecular shuttles having the structure (fusion protein)n-linker-(cargo)m wherein “fusion protein” is a proteinaceous binding entity fused to an enzyme-type protein for which specific substrates exist. The proteinaceous binding entity is designed to bind to a target structure in vitro or in vivo, for example a cellular receptor.
摘要翻译： 本发明涉及包含适当连接并进一步携带一个或多个货物实体的多个酶底物的化合物。 特别地，这样的化合物具有结构（底物）正接头（货物）m，其中“底物”是酶型蛋白质特异的底物; n为2以上; “接头”是由1至300个原子组成的连接单元; “货物”是一种药物，可由荧光检测器检测的标记物，磁共振成像（MRI），正电子发射断层扫描（PET）或闪烁扫描法，或可转化为药物或可检测标签的官能团; m为1以上。 本发明还涉及具有结构（融合蛋白）正连接体（货物）m的相应分子梭子，其中“融合蛋白”是与特定底物存在的酶型蛋白质融合的蛋白质结合实体。 蛋白质结合实体被设计为在体外或体内结合靶结构，例如细胞受体。
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公开(公告)号：US08623627B2
公开(公告)日：2014-01-07
申请号：US13484954
申请日：2012-05-31
IPC分类号： C12N9/12 , C07D239/47
CPC分类号： G01N33/581 , C07D239/47 , C07D403/14 , C07D405/12 , C07D487/04 , C12N9/12 , C12Q1/48
摘要： The invention relates to new proteins called alkylcytosine transferases (ACTs) derived from O6-alkylguanine-DNA alkyltransferase, and to substrates for ACTs specifically transferring a label to these ACTs and to fusion proteins comprising these. The substrates according of the invention are substituted cytosines of formula (I) wherein R1 is an aromatic or a heteroaromatic group, or an optionally substituted unsaturated alkyl, cycloalkyl or heterocyclyl group with the double bond connected to OCH2—; R2 is a linker; and L is a label or a plurality of same or different labels. The invention further relates to methods of transferring label L from these substrates of formula (I) to ACTs and ACT fusion proteins. The system of ACT-compound of formula (I) is particularly suitable for double labelling studies together with the known system O6-alkylguanine-DNA alkyltransferase (AGT)-benzylguanines.
摘要翻译： 本发明涉及从O6-烷基鸟嘌呤-DNA烷基转移酶衍生的称为烷基胞嘧啶转移酶（ACT）的新蛋白质，以及将这些ACT特异性转移标记物的ACT和包含这些酶的融合蛋白质的底物。 根据本发明的底物是其中R 1是芳族或杂芳族基团的式（I）的取代的胞嘧啶或具有与OCH 2连接的双键的任选取代的不饱和烷基，环烷基或杂环基; R2是连接体; L是标签或多个相同或不同的标签。 本发明还涉及将标记L从这些式（I）底物转移到ACT和ACT融合蛋白的方法。 式（I）的ACT-化合物的系统特别适用于已知的系统O6-烷基鸟嘌呤-DNA烷基转移酶（AGT） - 苄基胍的双重标记研究。
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