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Molecules 2015, 20(3), 4148-4161; doi:10.3390/molecules20034148

Tethering in RNA: An RNA-Binding Fragment Discovery Tool

1
Department of Chemistry, University of California, One Shields Ave, Davis, CA 95616, USA
2
Small Molecule Discovery Center, Department of Pharmaceutical Chemistry, University of California, San Francisco, CA 94158, USA
*
Author to whom correspondence should be addressed.
Academic Editors: Mahesh K. Lakshman and Fumi Nagatsugi
Received: 5 December 2014 / Revised: 20 January 2015 / Accepted: 17 February 2015 / Published: 4 March 2015
(This article belongs to the Special Issue Nucleoside Modifications)
View Full-Text   |   Download PDF [3613 KB, uploaded 4 March 2015]   |  

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. View Full-Text
Keywords: Tethering; miRNA; nucleoside analog Tethering; miRNA; nucleoside analog
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Tran, K.; Arkin, M.R.; Beal, P.A. Tethering in RNA: An RNA-Binding Fragment Discovery Tool. Molecules 2015, 20, 4148-4161.

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