Site-specific conjugation of drug-like fragments to an antimiR scaffold as a strategy to target miRNAs inside RISC

Chem Commun (Camb). 2016 Jan 4;52(1):156-9. doi: 10.1039/c5cc07478a.


We synthesized a miR-122 antimiR library in which drug-like fragments were site-specifically introduced to short 2'-O-methyl-RNAs. At some sites selected fragments elevated cellular antimiR activity to that of an unmodified 23mer antimiR, whereas at others the same fragments abolished activity. The potency of the antimiRs correlated with uptake into miRISC.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Base Sequence
  • Drug Discovery
  • Gene Silencing*
  • Humans
  • MicroRNAs / genetics*
  • MicroRNAs / metabolism
  • Models, Molecular
  • Neoplasms / genetics*
  • Neoplasms / metabolism
  • Oligoribonucleotides, Antisense / chemistry
  • Oligoribonucleotides, Antisense / genetics*
  • Oligoribonucleotides, Antisense / metabolism
  • RNA-Induced Silencing Complex / metabolism*


  • MIRN122 microRNA, human
  • MicroRNAs
  • Oligoribonucleotides, Antisense
  • RNA-Induced Silencing Complex