公开(公告)号：US20070243568A1

公开(公告)日：2007-10-18

申请号：US10591162

申请日：2005-03-01

申请人： Hughes Jaccard ,  Kai Johnsson ,  Maik Kindermann ,  India Christina Sielaff

发明人： Hughes Jaccard ,  Kai Johnsson ,  Maik Kindermann ,  India Christina Sielaff

IPC分类号： C07D473/18 ,  C12Q1/48

CPC分类号： C07D473/18

摘要： The invention relates to substrates for O6-alkylguanine-DNA alkyltransferases (AGT) of formula R1-A-X—CH2—R3—R4-L1, wherein A is a group recognized by AGT as a substrate, X is oxygen or sulfur, R1 is a group —R2-L2 or a group R5, R2 and R4 are, independently of each other, a linker, R3 is an aromatic or a heteroaromatic group, or an optionally substituted unsaturated alkyl, cycloalkyl or heterocyclyl group with the double bond connected to CH2, R5 is arylmethyl or heteroarylmethyl or an optionally substituted cycloalkyl, cycloalkenyl or heterocyclyl group, L1 is a label, a plurality of same or different labels, a bond connecting R4 to A forming a cyclic substrate, or a further group —R3 CH2—X-A-R1, and L2 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 O6-alkylguanine-DNA alkyltransferases (AGT) and AGT fusion proteins.

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; 1＆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-烷基鸟嘌呤-DNA烷基转移酶（AGT）和AGT融合蛋白的方法。

公开(公告)号：US08163479B2

公开(公告)日：2012-04-24

申请号：US10591162

申请日：2005-03-01

申请人： Hughes Jaccard ,  Kai Johnsson ,  Maik Kindermann ,  India Christina Sielaff

发明人： Hughes Jaccard ,  Kai Johnsson ,  Maik Kindermann ,  India Christina Sielaff

IPC分类号： C07D473/18 ,  C07D519/00 ,  C07D495/04 ,  C07D473/40

CPC分类号： C07D473/18

摘要： The invention relates to substrates for O6-alkylguanine-DNA alkyltransferases (AGT) of formula R1-A-X—CH2—R3—R4-L1, wherein A is a group recognized by AGT as a substrate, X is oxygen or sulfur, R1 is a group —R2-L2 or a group R5, R2 and R4 are, independently of each other, a linker, R3 is an aromatic or a heteroaromatic group, or an optionally substituted unsaturated alkyl, cycloalkyl or heterocyclyl group with the double bond connected to CH2, R5 is arylmethyl or heteroarylmethyl or an optionally substituted cycloalkyl, cycloalkenyl or heterocyclyl group, L1 is a label, a plurality of same or different labels, a bond connecting R4 to A forming a cyclic substrate, or a further group —R3—CH2—X-A-R1, and L2 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 O6-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为被AGT识别为底物的基团，X为氧或硫，R1为 基团-R2-L2或基团R5，R2和R4彼此独立地是连接基，R3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，其双键与CH2连接 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，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-R 3 -CH 2 - XA-R1和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。