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1. 发明申请

WO2005085470A9 SPECIFIC SUBSTRATES FOR O6- ALKYLGUANINE-DNA ALKYLTRANSFERASE 审中-公开
标题翻译：用于O6-氨基葡萄糖-DNA烷基转移酶的特异性底物
公开(公告)号：WO2005085470A9
公开(公告)日：2006-10-05
申请号：PCT/EP2005050900
申请日：2005-03-01
申请人： EPFL ECOLE POLYTECHNIQUE FEDERALE LAUSANNE , JACCARD HUGHES , JOHNSSON KAI , KINDERMANN MAIK , SIELAFF INDIA CHRISTINA
发明人： JACCARD HUGHES , JOHNSSON KAI , KINDERMANN MAIK , SIELAFF INDIA CHRISTINA
IPC分类号： C07D473/18 , C12Q1/48
CPC分类号： C07D473/18
摘要： The invention relates to substrates for O 6 -alkylguanine-DNA alkyltransferases (AGT) of formula R 1 -A-X-CH 2 -R 3 -R 4 -L 1 , wherein A is a group recognized by AGT as a substrate, X is oxygen or sulfur, R 1 is a group -R 2 -L 2 or a group R 5 , R 2 and R 4 are, independently of each other, a linker, R 3 is an aromatic or a heteroaromatic group, or an optionally substituted unsaturated alkyl, cycloalkyl or heterocyclyl group with the double bond connected to CH 2 , R 5 is arylmethyl or heteroarylmethyl or an optionally substituted cycloalkyl, cycloalkenyl or heterocyclyl group, L 1 is a label, a plurality of same or different labels, a bond connecting R 4 to A forming a cyclic substrate , or a further group -R 3 CH 2 -X-A-R 1, and L 2 is a label or a plurality of same or different labels. The invention further relates to methods of transferring a label from these substrates to O 6-
摘要翻译：本发明涉及式R 1 -AX-CH 2 -R Sub的O 6 - 烷基鸟嘌呤-DNA烷基转移酶（AGT）的底物其中A是被AGT识别为底物的基团，X是氧或硫，R 1 是基团-R 2→L 2或基团R 5，R 2和/或 R 4彼此独立地是连接基，R 3是芳族或杂芳族基团，或任选取代的不饱和烷基，环烷基或杂环基与双与CH 2 R 2连接的键是R 5是芳基甲基或杂芳基甲基或任选取代的环烷基，环烯基或杂环基，L 1是标记，多个相同或不同的标记，连接R 4与形成环状基底的A的键，或另外的基团-R 3 3 CH 2 -XAR 1，＆lt; / 2＆gt;和L 2 2是标签或多个相同或不同的标签。本发明还涉及将标记从这些底物转移到O6-6的方法

2. 发明申请

WO2005085470A1 SPECIFIC SUBSTRATES FOR O6- ALKYLGUANINE-DNA ALKYLTRANSFERASE 审中-公开
标题翻译： O 6 - 碱基 - DNA烷基转移酶的特异性底物
公开(公告)号：WO2005085470A1
公开(公告)日：2005-09-15
申请号：PCT/EP2005/050900
申请日：2005-03-01
申请人： EPFL ECOLE POLYTECHNIQUE FEDERALE DE LAUSANNE , JACCARD, Hughes , JOHNSSON, Kai , KINDERMANN, Maik , SIELAFF, India, Christina
发明人： JACCARD, Hughes , JOHNSSON, Kai , KINDERMANN, Maik , SIELAFF, India, Christina
IPC分类号： C12Q1/48
CPC分类号： C07D473/18
摘要： The invention relates to substrates for O 6 -alkylguanine-DNA alkyltransferases (AGT) of formula R 1 -A-X-CH 2 -R 3 -R 4 -L 1 , wherein A is a group recognized by AGT as a substrate, X is oxygen or sulfur, R 1 is a group -R 2 -L 2 or a group R 5 , R 2 and R 4 are, independently of each other, a linker, R 3 is an aromatic or a heteroaromatic group, or an optionally substituted unsaturated alkyl, cycloalkyl or heterocyclyl group with the double bond connected to CH 2 , R 5 is arylmethyl or heteroarylmethyl or an optionally substituted cycloalkyl, cycloalkenyl or heterocyclyl group, L 1 is a label, a plurality of same or different labels, a bond connecting R 4 to A forming a cyclic substrate , or a further group -R 3 CH 2 -X-A-R 1, and L 2 is a label or a plurality of same or different labels. The invention further relates to methods of transferring a label from these substrates to O 6- alkylguanine - DNA alkyltransferases (AGT) and AGT fusion proteins.
摘要翻译：本发明涉及式R1-AX-CH2-R3-R4-L1的O6 - 烷基鸟嘌呤-DNA烷基转移酶（AGT）的底物，其中A是被AGT识别为底物的基团，X是氧或硫， R 1是基团-R 2 -L 2或基团R 5，R 2和R 4彼此独立地是连接基，R 3是芳族或杂芳族基团，或具有双键的任选取代的不饱和烷基，环烷基或杂环基连接到CH2，R5是芳基甲基或杂芳基甲基或任选取代的环烷基，环烯基或杂环基，L1是标记，多个相同或不同的标记，连接R4与A形成环状底物的键或另外的基团-R3 CH2-XA-R1，L2是标签或多个相同或不同的标签。本发明还涉及将标记从这些底物转移到O6-烷基鸟嘌呤 - DNA烷基转移酶（AGT）和AGT融合蛋白的方法。

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