Assay Optimization and Screening of RNA-Protein Interactions by AlphaScreen

J Biomol Screen. 2007 Oct;12(7):946-55. doi: 10.1177/1087057107306128.


The lack of lead compounds that specifically recognize and manipulate the function of RNA molecules limits our ability to consider RNA targets valid for drug discovery. Herein is reported a high-throughput biochemical screen for inhibitors of RNA-protein interactions based on AlphaScreen technology that incorporates several layers of specificity measurements into the primary screen. This screen was used to analyze approximately 5500 compounds from a collection of bioactive small molecules to detect inhibitors of the HIV-1 Rev-RRE and BIV Tat-TAR interactions. This proof-of-concept screen validates the assay as one that accurately identifies hit molecules and determines the selectivity of those hits.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Base Sequence
  • Fluorescence Polarization / methods*
  • Protein Binding
  • RNA / metabolism*
  • RNA-Binding Proteins / metabolism*
  • Surface Plasmon Resonance


  • RNA-Binding Proteins
  • RNA