Aminoglycoside hybrids as potent RNA antagonists

Article abstract of DOI:10.1016/S0040-4020(99)00240-9

Aminoglycosides specifically bind to the A-site decoding region of prokaryotic 16S rRNA with dissociation constants in the 1-2 μM range. The aminoglycoside paromomycin binds to a truncated A-site construct with a K(d) = 1.85 μM. Paromomycin analogs are described here in which the aminoglycoside is linked via spacer groups to either thiazole orange or pyrene. These analogs bind specifically to the truncated A-site construct, but with affinities considerably higher than paromomycin itself. The binding of the hybrid molecules to the A-site is greater the shorter the spacer group.