利用两种正交高通量筛选技术对核糖体结合和抗菌活性进行表征。
Characterization of ribosomal binding and antibacterial activities using two orthogonal high-throughput screens.
机构信息
NUBAD, LLC, Greenville, South Carolina, USA.
出版信息
Antimicrob Agents Chemother. 2013 Oct;57(10):4717-26. doi: 10.1128/AAC.00671-13. Epub 2013 Jul 15.
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.
摘要
我们在此报告一类结构相似的新霉素二聚体的亲和力和抗菌活性。通过使用一种测量荧光素-新霉素（F-neo）探针从 RNA 中置换的筛选方法，确定了二聚体文库与 rRNA 的亲和力。使用单一药物浓度的快速生长抑制测定法来检查抗菌活性。然后使用二维核糖体结合-细菌抑制图分析快速分析结构-活性关系数据。
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