申请人:HISAMITSU PHARMACEUTICAL CO. INC.
公开号:EP1236736A1
公开(公告)日:2002-09-04
There are provided 2-aminopurine derivatives represented by the following general formula (1):
where R represents any species selected from the group consisting of hydrogen and acyl groups, X represents any species selected from the group consisting of phosphoramidite and oligonucleotides, Y represents any species selected from the group consisting of dimethyltrityl groups and oligonucleotides, and Z1, Z2, Z3, Z4 and Z5 are the same or different and represent any species selected from the group consisting of hydrogen and hydroxyl, amino, lower alkyl, alkoxy, carboxyl and sulfonic acid groups, provided that Z1, Z2, Z3, Z4 and Z5 are not all hydrogen,
as well as gene expression-regulating compositions characterized by comprising the derivatives. By introducing the 2-aminopurine derivatives into oligonucleotides it is possible to achieve crosslinking reaction with high reactivity for target nucleic acids and notably high base sequence specificity.
本发明提供了由以下通式(1)代表的 2-氨基嘌呤衍生物:
其中 R 代表选自由氢和酰基组成的组中的任何种类,X 代表选自由亚磷酰胺和寡核苷酸组成的组中的任何种类,Y 代表选自由二甲基三苯甲基和寡核苷酸组成的组中的任何种类、和 Z1、Z2、Z3、Z4 和 Z5 相同或不同,并代表选自由氢和羟基、氨基、低级烷基、烷氧基、羧基和磺酸基团组成的组中的任何种类,条件是 Z1、Z2、Z3、Z4 和 Z5 不全是氢、
以及基因表达调节组合物,其特征在于包含这些衍生物。通过在寡核苷酸中引入 2-氨基嘌呤衍生物,可以实现对目标核酸具有高反应活性和显著高碱基序列特异性的交联反应。