Antibacterial antisense oligonucleotide and method
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Abstract
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.
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18 Claims
- 1. A compound having the following formula (I):
- 8. An oligomer of 10 to 40 morpholino subunits connected by phosphorous-containing linkages of the formula:
- 10. A solid support covalently bound to a compound having the following structure:
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18. A compound of formula:
Specification