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Exploring eukaryotic versus prokaryotic ribosomal RNA recognition with aminoglycoside derivatives

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Abstract

New derivatives of aminoglycosides containing 6′-carboxylic acid or 6′-amide on their ring I were designed, synthesized and their ability to readthrough nonsense mutations was examined in vitro, along with the protein translation inhibition in prokaryotic and eukaryotic systems. The observed structure–activity relationships, along with the comparative molecular dynamics simulations within the eukaryotic rRNA decoding site, showed high sensitivity of 6′-position to substitution, indicating that the rational design of potent stop-codon read-through inducers requires consideration of not only the structure and energetics of the drug–RNA interaction but also the dynamics associated with that interaction.

Graphical abstract: Exploring eukaryotic versus prokaryotic ribosomal RNA recognition with aminoglycoside derivatives

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Publication details

The article was received on 01 Jan 2018, accepted on 31 Jan 2018 and first published on 02 Feb 2018


Article type: Research Article
DOI: 10.1039/C8MD00001H
Citation: Med. Chem. Commun., 2018, Advance Article
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    Exploring eukaryotic versus prokaryotic ribosomal RNA recognition with aminoglycoside derivatives

    N. M. Sabbavarapu, T. Pieńko, B. Zalman, J. Trylska and T. Baasov, Med. Chem. Commun., 2018, Advance Article , DOI: 10.1039/C8MD00001H

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