Journal
CHEMISTRY-A EUROPEAN JOURNAL
Volume 15, Issue 29, Pages 7109-7116Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.200802451
Keywords
aminoglycoside mimics; drug design; fragment-based synthesis; RNA recognition; tRNA
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A fragment-based approach for the synthesis of ligands of tRNA(3)(Lys), the HIV reverse-transcription primer, is described. The use of NMR spectroscopy has proved to be very useful in this approach, not only to detect low-affinity complexes between small compounds and RNA, but also to provide information on their binding mode and on the way they can be connected. This NMR-spectroscopy-guided analysis enabled us to design micromolar ligands after the optimisation and connection of millimolar fragments with an appropriate linker. The influence of the linker region on the binding affinity and selectivity outlines the importance of having a flexible assemblage strategy with a variety of linkers in such an approach.
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