System for delivering therapeutic agents into living cells and cells nuclei
The present invention relates to a novel delivery system for delivering therapeutic agents into living cells, and more particularly, to novel chemical moieties that are designed capable of targeting and/or penetrating cells or other targets of interest and further capable of binding therapeutic agents to be delivered to these cells, and to delivery systems containing same.
1. A conjugate of a phosphate based oligomeric compound with at least one biologically active substance, comprising a repeating unit represented by the structure of formula (A):
wherein
Y is a delivery group; wherein said delivery group is amine, histidine, guanidine, polyguanidine, imidazole, polyimidzole or any combination thereof; and
w, w′ and w″ are each independently an integer between 1 and 10;
wherein said biologically active substance is covalently attached to the terminus of said phosphate based oligomeric compound.
2. A complex of the conjugate according to claim 1 and an oligonucleotide, wherein said oligonucleotide, is electrostatically bound to said conjugate.
3. The complex according to claim 2 , wherein said oligonucleotide is DNA, RNA or combination thereof.
4. A method of delivering a DNA, RNA or combination thereof to a cell, said method comprises contacting a complex of claim 3 with said cell, thereby delivering said DNA, RNA or combination thereof to said cell.
5. The method of claim 4 , wherein said cell is cancerous.
6. A method of treating cancer, comprising administering a complex of claim 2 to a subject, thereby treating cancer.
7. A method of delivering a biologically active moiety to a cell, said method comprises contacting a conjugate of claim 1 with said cell, thereby delivering said biologically active moiety to said cell.
8. A method of diagnosing a condition, comprising contacting a conjugate of claim 1 with a cell, wherein said biologically active substance covalently attached to said conjugate is a labeling moiety, thereby delivering the labeling moiety of said conjugate to said cell and diagnosing said condition.
9. A pharmaceutical composition comprising the conjugate of claim 1 and a pharmaceutically acceptable carrier.
10. A pharmaceutical composition comprising the complex of claim 2 and a pharmaceutically acceptable carrier.
11. The conjugate of claim 1 , further comprising linker units, which link between repeating units of said conjugate, wherein said linker comprises a substituted or unsubstituted linear alkyl chain of 2-50 carbon atoms, substituted or unsubstituted linear or branched alkylphosphate chain of 2-50 carbon atoms, substituted or unsubstituted linear alkylether chain of 2-50 carbon atoms or any combination thereof.
12. A complex of the conjugate according to claim 11 and an oligonucleotide, wherein said oligonucleotide, is electrostatically bound to said conjugate.
13. A pharmaceutical composition comprising the complex of claim 2 and a pharmaceutically acceptable carrier.
14. The complex according to claim 12 , wherein said oligonucleotide is DNA, RNA or combination thereof.