Conjugates of oligonucleotides and analogues with cell penetrating peptides as gene silencing agents

T. S. Zatsepin, J. J. Turner, T. S. Oretskaya, M. J. Gait

Research output: Contribution to journalReview articlepeer-review

85 Citations (Scopus)

Abstract

The review describes key aspects of the synthesis and biological activities of conjugates of oligonucleotides and their analogues with synthetic peptides, in particular aimed towards gene silencing applications. The common methods of synthesis of oligonucleotide-peptide conjugates (OPCs) and PNA-peptide conjugates (PPCs) are described, which include both total solid-phase and fragment coupling approaches. In addition, various applications of conjugates as gene silencing agents are outlined. These include antisense and steric block applications in mammalian cells of OPCs, PPCs and phosphorodiamidate morpholinooligonucleotide (PMO)-peptide conjugates, gene silencing in bacteria, various DNA targeting applications, and recent reports of gene silencing activities of siRNA-peptide conjugates. A table listing all peptides used as oligonucleotide conjugates for gene silencing applications is also included.

Original languageEnglish
Pages (from-to)3639-3654
Number of pages16
JournalCurrent Pharmaceutical Design
Volume11
Issue number28
DOIs
Publication statusPublished - 2005
Externally publishedYes

Keywords

  • Antisense
  • Cell penetrating peptide
  • Conjugate
  • Gene silencing
  • Oligonucleotide

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