Antibacterial antisense oligonucleotide and method
AssigneeSarepta Therapeutics, Inc.
InventorsDwight D. Weller, Bruce L. Geller, Patrick L. Iversen, Lucas D. Tilley, Jed N. Hassinger
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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.
Claims22
1-20. (canceled)
A compound having the following formula (I):
- or a salt thereof, wherein:
- R1 is H, trityl or the 5′ terminal phosphorous of a morpholino oligomer;
- R2 is H or
- and
- R3 is H or a linkage to a solid support.
A morpholino oligomer comprising the following structure:
- wherein P1 represents the 5′ terminal phosphorous atom of the morpholino oligomer.
A solid support covalently bound to a compound having the following structure:
- wherein:
- R1 is H, trityl or the 5′ terminal phosphorous of a morpholino oligomer;
- and
- R3 is a linkage to the solid support.
Dependencies are inferred from the claim text.