title: Surface plasmon resonance evaluation of various aminoglycoside-RNA hairpin interactions reveals low degree of selectivity.
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.
authors.affiliation: Leiden Institute of Chemistry, Gorlaeus Laboratories, P. O. Box 9502, 2300 RA Leiden, The Netherlands.
authors.forename: Steven H L
authors.initials: SH
authors.lastname: Verhelst
authors.forename: Paul J A
authors.initials: PJ
authors.lastname: Michiels
authors.forename: Gijsbert A
authors.initials: GA
authors.lastname: van der Marel
authors.forename: Constant A A
authors.initials: CA
authors.lastname: van Boeckel
authors.forename: Jacques H
authors.initials: JH
authors.lastname: van Boom
mesh_terms: D000617:Aminoglycosides / Q000378:metabolism*; D000900:Anti-Bacterial Agents / Q000378:metabolism*; D020029:Base Pairing; D001483:Base Sequence; D004347:Drug Interactions; D005069:Evaluation Studies as Topic; D008969:Molecular Sequence Data; D009690:Nucleic Acid Conformation; D004364:Pharmaceutical Preparations; D012313:RNA / Q000737:chemistry* / Q000378:metabolism*; D020349:Surface Plasmon Resonance; D014031:Tobramycin / Q000737:chemistry / Q000378:metabolism
chemical_list: D000617:Aminoglycosides; D000900:Anti-Bacterial Agents; D004364:Pharmaceutical Preparations; D012313:RNA; D014031:Tobramycin