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    • 1. 发明申请
    • SPECIFIC SUBSTRATES FOR O6- ALKYLGUANINE-DNA ALKYLTRANSFERASE
    • 用于O6-氨基葡萄糖-DNA烷基转移酶的特异性底物
    • WO2005085470A9
    • 2006-10-05
    • PCT/EP2005050900
    • 2005-03-01
    • EPFL ECOLE POLYTECHNIQUE FEDERALE LAUSANNEJACCARD HUGHESJOHNSSON KAIKINDERMANN MAIKSIELAFF INDIA CHRISTINA
    • JACCARD HUGHESJOHNSSON KAIKINDERMANN MAIKSIELAFF INDIA CHRISTINA
    • C07D473/18C12Q1/48
    • C07D473/18
    • 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-
    • 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,< / 2>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