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New Approaches in Sensing and Targeting Bacterial rRNA A-site
Medicinal Chemistry ( IF 1.9 ) Pub Date : 2021-05-01 , DOI: 10.2174/1573406415666191011160035
Preethi Parameswaran 1 , Nihar Ranjan 1 , S.J.S. Flora 2
Affiliation  

New chemical agents that could combat increasing antibiotic resistance are urgently needed. In this mini-review, an old but highly relevant RNA sequence which is crucial for the continuation of bacterial life-cycle is covered. Some of the most significant advances of the last decade in sensing and targeting the bacterial rRNA A-site: a well-validated binding site of proverbially known aminoglycoside antibiotics are described. Some of the major advances in direct sensing of the bacterial decoding side (A-site) are described and also new fluorescent molecules that are capable of detecting lead compounds through high-throughput assays by displacement of fluorescent probe molecules are highlighted. Lastly, some of the recently discovered non-aminoglycoside small molecule binders of bacterial rRNA A-site as a new class of molecules that could provide future scaffolds and molecules for developing new antibacterial agents have been discussed.



中文翻译:

传感和靶向细菌rRNA A位点的新方法

迫切需要可以对抗日益增加的抗生素耐药性的新化学试剂。在此小型审查中,涵盖了一个古老但高度相关的RNA序列,该序列对于细菌生命周期的持续进行至关重要。过去十年中,在感知和靶向细菌rRNA A位点方面一些最重要的进展:描述了众所周知的氨基糖苷类抗生素的有效结合位点。描述了对细菌解码面(A部位)进行直接传感的一些主要进展,并着重介绍了能够通过置换荧光探针分子通过高通量检测来检测先导化合物的新型荧光分子。最后,

更新日期:2021-04-13
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