NMR-guided fragment-based approach for the design of tRNA(Lys3) ligands.
Résumé
Despite recent breakthroughs, the de novo design of new compounds that specifically bind to structured RNAs is still a standing challenge. The aim of this study was to find molecules that bind to tRNALys3 and serve as leads for inhibitors of the formation of the HIV-1 reverse transcription initiation complex. We used NMR screening to identify ligands from spectral changes induced by their binding on the target. Using a fragment-based approach, a selective ligand of tRNALys3 with micromolar dissociation constant has been synthesised for the first time.
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