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PMID: 15239050 Published · ppublish English Journal Article

Surface plasmon resonance evaluation of various aminoglycoside-RNA hairpin interactions reveals low degree of selectivity.

Chembiochem : a European journal of chemical biology ·Vol. 5 ·No. 7 ·2004-07-05 ·Pages 937-42

Verhelst SH, Michiels PJ, van der Marel GA, van Boeckel CA, van Boom JH

Abstract

Aminoglycoside antibiotics, which are able to selectively bind to RNA, are considered to be an important lead in RNA-targeting drug discovery. In this study, surface plasmon resonance (SPR) was employed to explore the interaction of aminoglycosides with known tobramycin-binding RNA hairpins (aptamers) and an unrelated RNA hairpin. It was established that aminoglycosides have multiple interactions with RNA hairpins. Unexpectedly, the different hairpins showed comparable affinity for a set of related aminoglycosides. The observed absence of selectivity presents an extra hurdle in the discovery of novel aminoglycosides as specific drugs that target defined RNA hairpins.

MeSH Terms
Aminoglycosides/metabolism Anti-Bacterial Agents/metabolism Base Pairing Base Sequence Drug Interactions Evaluation Studies as Topic Molecular Sequence Data Nucleic Acid Conformation Pharmaceutical Preparations RNA/chemistry,metabolism Surface Plasmon Resonance Tobramycin/chemistry,metabolism
Chemicals
Aminoglycosides Anti-Bacterial Agents Pharmaceutical Preparations RNA Tobramycin
Authors & Affiliations
5 authors, click to expand affiliations / ORCID
Verhelst Steven H L
Leiden Institute of Chemistry, Gorlaeus Laboratories, P. O. Box 9502, 2300 RA Leiden, The Netherlands.
Michiels Paul J A
van der Marel Gijsbert A
van Boeckel Constant A A
van Boom Jacques H
Article Info
Journal
Chembiochem : a European journal of chemical biology
Abbr.
Chembiochem
ISSN
1439-4227
Published
2004-07-05
Pages
937-42
Language
English
Region
Germany
NLM ID
100937360
Subset
IM
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