Gapped 2' modified oligonucleotides
AssigneeIsis Pharmaceuticals, Inc.
InventorsPhillip Dan Cook, Brett P. Monia
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Abstract
Oligonucleotides and other macromolecules are provided which have increased nuclease resistance, substituent groups for increasing binding affinity to complementary strand, and subsequences of 2'-deoxy-erythro-pentofuranosyl nucleotides that activate RNase H. Such oligonucleotides and macromolecules are useful for diagnostics and other research purposes, for modulating the expression of a protein in organisms, and for the diagnosis, detection and treatment of other conditions susceptible to oligonucleotide therapeutics.
Claims15
An oligonucleotide comprising a sequence of nucleotide unite specifically hybridizable with DNA or RNA wherein said sequence is divided into a first segment and a second segment, wherein:
- said first segment is adjacent said second segment and does not overlap said second segment;
- said first segment has at least two consecutively located 2'-F nucleotide units;
- said second segment is composed of at least five consecutively located nucleotide units having 2'-H sugar moieties;
- and
- said oligonucleotide hybridizes with said DNA or RNA with higher binding affinity than a corresponding oligomer in which said at least two consecutively located 2'-F nucleotide units are 2'-H nucleotide units.
An oligonucleotide comprising a sequence of nucleotide units specifically hybridizable with DNA or RNA, wherein said sequence is divided into a first segment, a second segment, and a third segment wherein:
- said first segment and said third segment each has at least two consecutively located 2'-deoxy-2'-fluoro nucleotide units;
- and
- said second segment is positioned adjacent to and between said first segment and said third segment and is composed of at least three consecutively located nucleotide units having 2'-deoxy sugar moieties.
Dependencies are inferred from the claim text.