Single chemical entities and methods for delivery of oligonucleotides
View Patent ↗In an embodiment the instant invention discloses a modular composition comprising 1) an oligonucleotide; 2) one or more linkers, which may be the same or different, selected from Table 1, wherein the linkers are attached to the oligonucleotide at any 3′ and/or 5′ end; 3) one or more peptides, which may be the same or different, selected from SEQ ID NOs: 1-59, wherein the peptides are attached to the linkers; and optionally one or more lipids, solubilizing groups and/or targeting ligands attached to the oligonucleotide.
1. A modular composition comprising 1) an siRNA; 2) one or more linkers, which may be the same or different, selected from the following linkers, wherein the linkers are attached to the siRNA at any 3′ and/or 5′ end;
and n=0 to 750;
and 3) one or more peptides, which may be the same or different, selected from SEQ ID NOs 1-59, wherein the peptides are attached to the linkers.
2. The modular composition of claim 1 wherein the linkers are attached to the guide strand of the siRNA at the 3′ and/or 5′ end.
3. The modular composition of claim 1 wherein the linkers are attached to the passenger strand of the siRNA at the 3′ and/or 5′ end.
4. A modular composition comprising 1) an siRNA; 2) one or more linkers, which may be the same or different, selected from the following linkers, wherein the linkers are attached to the siRNA at any 3′ and/or 5′ end;
and n=0 to 750;
and 3) one or more peptides, which may be the same or different, selected from SEQ ID NOs: 28, 29, 33, 35, 36, 40, 50, 51, 52, 53, 54, 55, 56, 57, 58, and 59, wherein the peptides are attached to the linkers.
5. The modular composition of claim 4 wherein the linkers are attached to the guide strand of the siRNA at the 3′ and/or 5′ end.
6. The modular composition of claim 4 wherein the linkers are attached to the passenger strand of the siRNA at the 3′ and/or 5′ end.