Methods to assay inhibitors of tRNA synthetase activity.

Dieter Beyer, Hein Peter Kroll, Heike Brötz-Oesterhelt
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引用次数: 1

Abstract

Aminoacyl-tRNA synthetases (aa-RS) attracted interest as potential targets for new antibacterial compounds. Most organisms express 20 aa-RSs: one for each amino acid. Aa-RSs are essential proteins in all living organisms. When one aa-RS is inhibited, the corresponding tRNA is not charged and is therefore unavailable for translation. This leads to protein synthesis inhibition, which in turn causes cell growth arrest. Consequently, each compound that inhibits any of the aa-RS could be a potential antibacterial agent. Only one aa-RS inhibitor, the Ile-RS inhibitor mupirocin, is currently marketed as an antibacterial agent. We focused on phenylalanyl (Phe)-tRNA synthetase (Phe-RS), but the described methods are not restricted to Phe-RS and might be adapted to other aa-RS.

方法测定tRNA合成酶活性抑制剂。
氨基酰基trna合成酶(aa-RS)作为新型抗菌化合物的潜在靶点引起了人们的兴趣。大多数生物体表达20个aa-RSs:每个氨基酸一个。Aa-RSs是所有生物体内必需的蛋白质。当一个aa-RS被抑制时,相应的tRNA不带电,因此无法翻译。这导致蛋白质合成抑制,进而导致细胞生长停滞。因此,每种抑制aa-RS的化合物都可能成为潜在的抗菌剂。目前只有一种aa-RS抑制剂,即Ile-RS抑制剂莫匹罗星作为抗菌剂上市。我们的重点是苯丙酰(Phe)-tRNA合成酶(Phe- rs),但所描述的方法并不局限于Phe- rs,可能适用于其他aa-RS。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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