NOVEL OLIGONUCLEOTIDE CONJUGATES AND USE THEREOF

摘要

The present invention provides a double helix oligo-RNA structure in which target-specific ligands are bonded to the double helix oligo-RNA structure in which high molecular compounds for improving the delivery of double helix oligo-RNA that can be valuably used in treating diseases, specifically, cancer, are covalently bonded. The present invention also provides a method for preparing the RNA structure and a target-specific double helix oligo-RNA delivery technology through said structure. Nanoparticles constituted by the double helix oligo-RNA structure to which ligands are bonded may efficiently deliver double helix oligo-RNA to a target, and thus may exhibit an activity of double helix oligo-RNA structure in a target cell even with an administration of double helix oligo-RNA of relatively lower concentration. The nanoparticles may prevent the delivery of non-specific double helix oligo-RNA to other organs and cells, and therefore, can be valuably used not only as a tool for double helix oligo-RNA for treating various diseases, specifically, cancer, but also as a new type of double helix oligo-RNA delivery system. The present invention also relates to hybrid conjugates in which a hydrophilic material and a hydrophobic material are connected to both ends of antisense oligonucleotide(ASO) through covalent bond so as to achieve in vivo stability of the ASO, and to a method for preparing the hybrid conjugates and to nanoparticles constituted by the conjugates. The conjugates between ASO and macromolecules according to the present invention may improve in vivo stability of ASO, and therefore, can efficiently deliver ASO for treatment into cells and may exhibit an activity of ASO even with an administration of a relatively lower concentration.