Tethering in RNA: An RNA-Binding Fragment Discovery Tool

Tethering in RNA: An RNA-Binding Fragment Discovery Tool

Tethering has been extensively used to study small molecule interactions with proteins through reversible disulfide bond forming reactions to cysteine residues. We describe the adaptation of Tethering to the study of small molecule binding to RNA using a thiol-containing adenosine analog (ASH). Amon...

Full description

Bibliographic Details
Main Authors: Kiet Tran, Michelle R. Arkin, Peter A. Beal
Format: Article
Language:English
Published: MDPI AG 2015-03-01
Series:Molecules
Subjects:
Tethering
miRNA
nucleoside analog
Online Access:http://www.mdpi.com/1420-3049/20/3/4148
Description
Summary:Tethering has been extensively used to study small molecule interactions with proteins through reversible disulfide bond forming reactions to cysteine residues. We describe the adaptation of Tethering to the study of small molecule binding to RNA using a thiol-containing adenosine analog (ASH). Among 30 disulfide-containing small molecules screened for efficient Tethering to ASH-bearing RNAs derived from pre-miR21, a benzotriazole-containing compound showed prominent adduct formation and selectivity for one of the RNAs tested. The results of this screen demonstrate the viability of using thiol-modified nucleic acids to discover molecules with binding affinity and specificity for the purpose of therapeutic compound lead discovery.
ISSN:1420-3049

Similar Items