申请人:Sarepta Therapeutics, Inc.
公开号:US20140213737A1
公开(公告)日:2014-07-31
A method for enhancing, by at least 10 fold, the antibacterial activity of an antisense oligonucleotide composed of morpholino subunits linked by phosphorus-containing intersubunit linkages. The method includes one or both of: conjugating an arginine-rich carrier to a 3′ or 5′ end of the oligonucleotide and modifying the oligonucleotide to contain 20%-50% intersubunit linkages that are positively charged at physiological pH. Also disclosed is an antisense oligonucleotide having enhanced antibacterial activity by virtue of one or both modifications.
一种增强抗菌活性的反义寡核苷酸方法,其由连接磷含有的亚单位的Morpholino亚单位组成,能够至少增强10倍。该方法包括以下一种或两种:将富含精氨酸的载体与寡核苷酸的3'端或5'端结合,以及修改寡核苷酸,使其在生理pH下含有20%-50%的亚单位链接呈正电荷。此外,还公开了一种通过一种或两种修改具有增强抗菌活性的反义寡核苷酸。