Tumor-targeted Delivery of Anti-microRNA for Cancer Therapy: pHLIP is Key

Angew Chem Int Ed Engl. 2015 May 11;54(20):5824-6. doi: 10.1002/anie.201502146. Epub 2015 Apr 17.

Abstract

pHLIP opens the door to the cell: An improved cytosolic transfer of anti-microRNAs (anti-miRs) against onco-miRs paves the way for future cancer therapies. The employed anti-miR-peptide conjugates are based on peptide nucleic acids (PNAs), which are connected with the membrane translocation peptide pHLIP through a disulfide bond. The PNAs are thus transferred into the cell and released by the cleavage of the S-S bond.

Keywords: RNA; membranes; microRNA; peptide nucleic acids; targeted delivery.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Drug Delivery Systems*
  • Humans
  • Hydrogen-Ion Concentration
  • Mice
  • Mice, Nude
  • MicroRNAs / antagonists & inhibitors*
  • MicroRNAs / genetics
  • MicroRNAs / metabolism
  • Neoplasms / drug therapy*
  • Neoplasms / genetics
  • Neoplasms / metabolism*
  • Peptide Nucleic Acids / chemistry
  • Peptide Nucleic Acids / metabolism*
  • Peptide Nucleic Acids / pharmacology*
  • Peptides / chemistry*

Substances

  • MicroRNAs
  • Peptide Nucleic Acids
  • Peptides