Tethering in RNA: An RNA-binding fragment discovery tool

Kiet Tran, Michelle R. Arkin, Peter A. Beal

Research output: Contribution to journalArticle

Abstract

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.

Original languageEnglish (US)
Pages (from-to)4148-4161
Number of pages14
JournalMolecules
Volume20
Issue number3
DOIs
StatePublished - Mar 1 2015

Keywords

  • miRNA
  • Nucleoside analog
  • Tethering

ASJC Scopus subject areas

  • Organic Chemistry

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