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Combinatorial Chemistry & High Throughput Screening

Editor-in-Chief

ISSN (Print): 1386-2073
ISSN (Online): 1875-5402

Establishment of a Primary Screening Assay for the DHX9 Helicase

Author(s): Regina Cencic, Patrick Senechal and Jerry Pelletier

Volume 18 , Issue 9 , 2015

Page: [855 - 861] Pages: 7

DOI: 10.2174/1386207318666151019093433

Price: $65

Abstract

The RNA helicase DHX9 is an ATP-dependent DExH box helicase that can unwind DNA and RNA. Much evidence has implicated DHX9 at multiple levels of gene expression regulation ranging from genome stability and replication, to transcriptional control and translation regulation. Its association with the EWS-FLI1 fusion product, as well as the finding that its suppression can be synthetic lethal with the BCL-2 family inhibitor ABT-737 indicates a potential role in tumor maintenance. Hence, to identify small molecules that could interfere with its activity, we developed a homogenous RNA-dependent ATPase assay. We show that aurintricarboxylic acid, a promiscuous protein-nucleic acid inhibitor prevents DHX9-mediated hydrolysis demonstrating that the assay is also capable of detecting compounds that impinge on DHX9:RNA association.

Keywords: ATPase assay, ATA, aurintricarboxylic acid, DHX9, HTS, RNA binding, RNA helicase.


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