Selective inhibition of miR-21 by phage display screened peptide

Nucleic Acids Res. 2015 Apr 30;43(8):4342-52. doi: 10.1093/nar/gkv185. Epub 2015 Mar 30.


miRNAs are nodal regulators of gene expression and deregulation of miRNAs is causally associated with different diseases, including cancer. Modulation of miRNA expression is thus of therapeutic importance. Small molecules are currently being explored for their potential to downregulate miRNAs. Peptides have shown to have better potency and selectivity toward their targets but their potential in targeting and modulating miRNAs remain unexplored. Herein, using phage display we found a very selective peptide against pre-miR-21. Interestingly, the peptide has the potential to downregulate miR-21, by binding to pre-miR-21 and hindering Dicer processing. It is selective towards miR-21 inside the cell. By antagonising miR-21 function, the peptide is able to increase the expression of its target proteins and thereby increase apoptosis and suppress cell proliferation, invasion and migration. This peptide can further be explored for its anti-cancer activity in vivo and may be even extended to clinical studies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / metabolism
  • Antineoplastic Agents / pharmacology*
  • Apoptosis
  • Binding Sites
  • Cell Line
  • Cell Movement / drug effects
  • Cell Proliferation / drug effects
  • Cell Surface Display Techniques
  • MCF-7 Cells
  • MicroRNAs / antagonists & inhibitors*
  • MicroRNAs / chemistry
  • MicroRNAs / metabolism
  • Neoplasm Invasiveness
  • Neoplasms / pathology
  • Nucleotides / chemistry
  • Peptides / chemistry
  • Peptides / metabolism
  • Peptides / pharmacology*
  • RNA Precursors / metabolism


  • Antineoplastic Agents
  • MIRN21 microRNA, human
  • MicroRNAs
  • Nucleotides
  • Peptides
  • RNA Precursors