RNA interference with chemically modified siRNA

Hong Yan Zhang, Quan Du, Claes Wahlestedt, Zicai Liang

Research output: Contribution to journalReview articlepeer-review

34 Scopus citations


siRNA has become an indispensable tool for functional characterization of genes. It has also demonstrated tremendous potential as a new generation of drug candidates. Although the technology works very well to a great panel of cells in vitro, it is still a challenge to translate the success into in vivo target validation easiness and, even more difficult, into therapeutic applications. With a number of chemically modified compounds under initial clinical trial from several commercial entities, the interests in chemical modification of siRNA have become heightened. In this review we have tried to touch on most of the chemical modifications of RNA that have been tested in the siRNA landscape, but maintained a focus on the backbone modifications, and 2′-modifications on the ribose ring. It is anticipated that more modifications and more systematic comparisons between different modifications will be performed to draw more educated conclusions over some of the modifications.

Original languageEnglish (US)
Pages (from-to)893-900
Number of pages8
JournalCurrent Topics in Medicinal Chemistry
Issue number9
StatePublished - May 1 2006
Externally publishedYes


  • Backbone modifications
  • Lactosylated-PEG-siRNA conjugates
  • Oligonucleotides
  • RNA sugar ring
  • Terminal modifications

ASJC Scopus subject areas

  • Medicine(all)
  • Chemistry(all)


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