Fig. 7: MraY inhibitory activity of SPMs.
From: Synthesis of macrocyclic nucleoside antibacterials and their interactions with MraY
a The inhibitory activities of the compounds against purified MraYAA. Assays were conducted with 100 mM Tris-HCl, 500 mM NaCl, 10 mM MgCl2, and 20 mM (3-((3-cholamidopropyl) dimethylammonio)-1-propanesulfonate), 150 μM UDP-MurNAc-pentapeptide, 250 μM C55-P, and MraYAA (50 nM). After 5 min of incubation at 45 °C, the formation of UMP was monitored by luminescence measurement. b The inhibitory activities of the compounds against purified MraYSA. Assays were conducted with 50 mM Tris-HCl (pH 7.6), 50 mM KCl, 25 mM MgCl2, 0.2% Triton X-100, 8% glycerol, 50 μM C55-P, 10 μM UDP-MurNAc-dansylpentapeptide, and MraY enzyme (11 μg/mL, 5 μL/well). After 3–4 h incubation at room temperature, the formation of dansylated lipid I was monitored by fluorescence enhancement (excitation at 355 nm, emission at 535 nm). The data were obtained from three independent experiments and represented as mean ± SD. SPM-1 is shown in orange, SPM-2 is shown in blue, and SPM-3 is shown in green throughout.
