title: Characterization of ribosomal binding and antibacterial activities using two orthogonal high-throughput screens.
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.
authors.affiliation: NUBAD, LLC, Greenville, South Carolina, USA.
authors.forename: Ada
authors.initials: A
authors.lastname: King
authors.forename: Derrick
authors.initials: D
authors.lastname: Watkins
authors.forename: Sunil
authors.initials: S
authors.lastname: Kumar
authors.forename: Nihar
authors.initials: N
authors.lastname: Ranjan
authors.forename: Changjun
authors.initials: C
authors.lastname: Gong
authors.forename: Jarred
authors.initials: J
authors.lastname: Whitlock
authors.forename: Dev P
authors.initials: DP
authors.lastname: Arya
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology*; D016972:Enterobacter cloacae / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009355:Neomycin / Q000737:chemistry / Q000494:pharmacology; D011550:Pseudomonas aeruginosa / Q000187:drug effects; D012270:Ribosomes / Q000737:chemistry*; D012706:Serratia marcescens / Q000187:drug effects; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D009355:Neomycin