Efficient siRNA-peptide conjugation for specific targeted delivery into tumor cells

Despite the broad applicability of the Huisgen cycloaddition reaction, the click functionalization of RNAs with peptides remains still a challenge. Here we describe a straightforward method for the click functionalization of siRNAs with peptides of different size and complexity. Among them, a promising peptide carrier for the selective siRNA delivery into HER2+ breast cancer cell lines.