Assay optimization and screening of RNA-protein interactions by alphascreen

Nicholas L. Mills, Anang A. Shelat, R. Kiplin Guy

Research output: Contribution to journalArticlepeer-review

36 Scopus citations


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.

Original languageEnglish
Pages (from-to)946-955
Number of pages10
JournalJournal of Biomolecular Screening
Issue number7
StatePublished - Sep 2007


  • Bovine immunodeficiency virus
  • Fluorescence polarization
  • HIV-1 Rev
  • Rev-responsive element

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biotechnology
  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery


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