Dwight D. Weller,Bruce L. Geller,Patrick L. Iversen,Lucas D. Tilley,Jed N. Hassinger
申请号:
US13963919
公开号:
US09249243B2
申请日:
2013.08.09
申请国别(地区):
US
年份:
2016
代理人:
摘要:
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.