Fluorescent indicator displacement assay of ligands targeting 10 microRNA precursors

Bioorg Med Chem. 2013 Nov 15;21(22):7101-6. doi: 10.1016/j.bmc.2013.09.007. Epub 2013 Sep 14.

Abstract

Fluorescent indicator displacement (FID) assay is a rapid and convenient assay for identifying new ligands that bind to the target molecules. In our previous studies, we have shown that a series of 2,7-diaminoalkoxy xanthone and thioxanthone derivatives can be used as fluorescent indicators for detecting the interaction between RNA and a ligand. The xanthone and thioxanthone fluorochromes showed efficient fluorescence quenching upon binding to target RNA. Subsequent displacement of the bound-fluorochrome with a ligand that binds more strongly to the target RNA led to the recovery of the fluorescence by releasing the fluorochrome from RNA. Here we report a pilot screening of a chemical library that contains 9600 structurally diverse compounds for molecules that bind to a specific miRNA precursor using the FID assay.

Keywords: FID assay; Fluorescent indicator; Pre-miRNA; Screening; Small molecule.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Base Sequence
  • Fluorescent Dyes / chemistry*
  • Ligands*
  • MicroRNAs / analysis*
  • MicroRNAs / metabolism
  • RNA Precursors / analysis
  • RNA Precursors / metabolism
  • Spectrometry, Fluorescence
  • Xanthones / chemistry

Substances

  • Fluorescent Dyes
  • Ligands
  • MicroRNAs
  • RNA Precursors
  • Xanthones
  • xanthone