Characterization of Ribosomal Binding and Antibacterial Activities Using Two Orthogonal High-Throughput Screens |
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| Authors: | Ada King Derrick Watkins Sunil Kumar Nihar Ranjan Changjun Gong Jarred Whitlock Dev P. Arya |
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| Affiliation: | NUBAD, LLC, Greenville, South Carolina, USAa;Department of Chemistry, Clemson University, Clemson, South Carolina, USAb |
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| Abstract: | We report here the affinity and antibacterial activity of a structurally similar class of neomycin dimers. The affinity of the dimer library for rRNA was established by using a screen that measures the displacement of fluorescein-neomycin (F-neo) probe from RNA. A rapid growth inhibition assay using a single drug concentration was used to examine the antibacterial activity. The structure-activity relationship data were then rapidly analyzed using a two-dimensional ribosomal binding-bacterial inhibition plot analysis. |
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