Antibacterial antisense oligonucleotide and method

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.

主权项

1. A compound having the following formula (I):or a salt thereof, wherein:
R1 is H or trityl; R2 is H orand
R3 is H or a linkage to a solid support.