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US 11,696,954 B2Granted
Synthesis of spherical nucleic acids using lipophilic moieties
AssigneeExicure Operating Company
InventorsRichard Kang, Subbarao Nallagatla, Bart Anderson, Ekambar Kandimalla
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Abstract
Spherical nucleic acids (SNA) carrying self-aggregating oligonucleotides are described herein. Compositions of the SNA include discrete nanostructures that are not aggregated. Related methods are also described.
Claims13
A nanostructure comprising:
- a spherical nucleic acid (SNA) comprising a core, a lipid shell having an inner surface surrounding the core and an outer surface, and an oligonucleotide linked to a lipophilic moiety wherein the oligonucleotide is functionalized to the lipid shell through interaction between the lipid shell and at least a portion of the lipophilic moiety and the oligonucleotide is oriented radially outwards, wherein the lipophilic moiety is comprised of two or more lipophilic groups and has the following structure:
- -L1-(Spacer)n-L2-(Spacer)n1-L3-X-(alkyl group)m,
- wherein L1, L2, and L3 are each linkers and independent of one another are a phosphodiester or phosphorothioate bond or short chain linkage, wherein the spacer is an oligoethylene glycol spacer, wherein n and n1 are independently 0-3, wherein at least one of n and n1 is not 0, wherein X is a doubler or trebler, the alkyl group is a C6-C30 saturated or unsaturated alkyl group and m is 2-3, wherein the doubler and trebler have the following structures, respectively:
Dependencies are inferred from the claim text.