Use of a fluorescence assay to determine relative affinities of semisynthetic aminoglycosides to small RNAs representing bacterial and mitochondrial A sites.
Use of a fluorescence assay to determine relative affinities of semisynthetic aminoglycosides to small RNAs representing bacterial and mitochondrial A sites.
复制标题
使用荧光测定法测定半合成氨基糖苷类与代表细菌和线粒体 A 位点的小 RNA 的相对亲和力。
DOI：
10.1016/j.bmc.2019.115121
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发表时间：
2019
影响因子：
3.5
通讯作者：
Chow,ChristineS
中科院分区：
文献类型：
--
作者：
Waduge,Prabuddha;Sati,GirishC;Crich,David;Chow,ChristineS
除了细菌核糖体之外，氨基糖苷类（AG）与人线粒体核糖体的A位点的脱靶结合引起耳毒性并限制其作为抗生素的潜力。采用荧光测定来确定经典和改进的AG化合物与代表细菌和线粒体A位点的合成RNA构建体的相对结合亲和力。结果与以前报道的工程核糖体的体外翻译试验进行了比较。因此，最小的RNA基序和荧光测定在这里显示用于评估新化合物的选择性。
The off-target binding of aminoglycosides (AGs) to the A site of human mitochondrial ribosomes in addition to bacterial ribosomes causes ototoxicity and limits their potential as antibiotics. A fluorescence assay was employed to determine relative binding affinities of classical and improved AG compounds to synthetic RNA constructs representing the bacterial and mitochondrial A sites. Results compared well with previously reported in vitro translation assays with engineered ribosomes. Therefore, the minimal RNA motifs and fluorescence assay are shown here to be useful for assessing the selectivity of new compounds.