Modified iRNA agents
First Claim
1. An iRNA agent comprising a first strand and a second strand, wherein at least one one subunit having a formula (I) is incorporated into at least one of said strands:
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Abstract
The invention relates to iRNA agents, which preferably include a monomer in which the ribose moiety has been replaced by a moiety other than ribose. The inclusion of such a monomer can allow for modulation of a property of the iRNA agent into which it is incorporated, e.g., by using the non-ribose moiety as a point to which a ligand or other entity, e.g., a lipophilic moiety. e.g., cholesterol, is is directly, or indirectly, tethered. The invention also relates to methods of making and using such modified iRNA agents.
310 Citations
89 Claims
- 1. An iRNA agent comprising a first strand and a second strand, wherein at least one one subunit having a formula (I) is incorporated into at least one of said strands:
- 40. An iRNA agent comprising a first strand and a second strand, wherein at least one subunit is derivatized with a lipophilic moiety which enhances entrance into a cell.
- 79. A method of silencing a target gene comprising providing an iRNA agent, to which a lipophilic moiety is conjugated, to a cell.
- 85. A composition comprising an iRNA agent to which a lipophilic moiety is conjugated, which is free of, has a reduced amount of, or is essentially free of, other reagents that facilitate or enhance delivery through the cell membrane.
Specification