A solid-phase method for peptide–siRNA covalent conjugates based on click chemistry

Abstract

In order to prepare a new delivery system by chemical modification, peptide–siRNA conjugates have been obtained by a solid-phase click chemistry strategy, using an alkynyl nucleoside analogue “clicked” onto a peptide-derivatized CPG (Controlled Pore Glass) followed by oligonucleotides synthesis. The 3′-sense strand conjugate maintained good gene silencing activity, while that of the 3′-antisense strand conjugate decreased somewhat.