Open AccessAssay Optimization and Screening of RNA-Protein Interactions by AlphaScreen
Author(s) -
Nicholas L. Mills,
Anang A. Shelat,
R. Kiplin Guy
Publication year - 2007
Publication title -
slas discovery
Language(s) - English
Resource type - Journals
eISSN - 2472-5560
pISSN - 2472-5552
DOI - 10.1177/1087057107306128
Subject(s) - rna , drug discovery , small molecule , computational biology , function (biology) , high throughput screening , chemistry , biology , combinatorial chemistry , biochemistry , microbiology and biotechnology , gene
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.