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Issue 7, 2014
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Methods to enable the design of bioactive small molecules targeting RNA

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Abstract

RNA is an immensely important target for small molecule therapeutics or chemical probes of function. However, methods that identify, annotate, and optimize RNA-small molecule interactions that could enable the design of compounds that modulate RNA function are in their infancies. This review describes recent approaches that have been developed to understand and optimize RNA motif-small molecule interactions, including structure–activity relationships through sequencing (StARTS), quantitative structure–activity relationships (QSAR), chemical similarity searching, structure-based design and docking, and molecular dynamics (MD) simulations. Case studies described include the design of small molecules targeting RNA expansions, the bacterial A-site, viral RNAs, and telomerase RNA. These approaches can be combined to afford a synergistic method to exploit the myriad of RNA targets in the transcriptome.

Graphical abstract: Methods to enable the design of bioactive small molecules targeting RNA

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Publication details

The article was received on 22 Jan 2013, accepted on 18 Nov 2013 and first published on 21 Nov 2013


Article type: Review Article
DOI: 10.1039/C3OB42023J
Citation: Org. Biomol. Chem., 2014,12, 1029-1039
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    Methods to enable the design of bioactive small molecules targeting RNA

    M. D. Disney, I. Yildirim and J. L. Childs-Disney, Org. Biomol. Chem., 2014, 12, 1029
    DOI: 10.1039/C3OB42023J

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