申请人:Lukhtanov Eugeny A.
公开号:US20100137614A1
公开(公告)日:2010-06-03
The present invention provides a negatively charged minor groove binding compound, oligonucleotide conjugates comprising the same, and methods for using the same. The negatively charged minor groove binding compounds of the present invention comprises an acidic moiety that is capable of being ionized under physiological conditions. In particular, the negatively charged minor groove binding compound of the present invention comprises a binding moiety that binds preferentially into a minor groove of a double, triple or higher stranded DNA, RNA, PNA or hybrids thereof. The binding moiety comprises at least one aryl moiety and an acidic moiety which is covalently attached to a phenyl portion of the aryl moiety or to a heteroatom of a heteroaryl portion of the aryl moiety.
本发明提供了一种带有负电荷的小沟结合化合物,包括该化合物的寡核苷酸共轭物,并提供了使用它们的方法。本发明的带有负电荷的小沟结合化合物包括一个酸性基团,在生理条件下能够被电离。特别地,本发明的带有负电荷的小沟结合化合物包括一个结合基团,优先结合于双链、三链或更高链的DNA、RNA、PNA或其杂交物的小沟中。结合基团包括至少一个芳基基团和一个酸性基团,该酸性基团共价连接到芳基基团的苯基部分或芳基基团的杂环部分的杂原子上。