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论核糖体中抗生素结合位点的性质

On the nature of antibiotic binding sites in ribosomes.

作者信息

Cundliffe E

机构信息

Department of Biochemistry, University of Leicester, England.

出版信息

Biochimie. 1987 Aug;69(8):863-9. doi: 10.1016/0300-9084(87)90213-6.

Abstract

The ribosome is an enzyme and enzymes have active sites. Antibiotics that affect ribosomal function can be considered as enzyme inhibitors (or regulators) and it is therefore pertinent to identify their molecular targets as a means of studying the active sites of the particle. The methods available for doing this are considered and, in general terms, the data are evaluated. The conclusion is reached that there exists virtually no compelling evidence that antibiotics bind primarily to ribosomal proteins. Rather, studies of antibiotic resistance in various systems strongly suggest that ribosomal RNA is the primary target for a number of drugs. Moreover, in at least one case (relating to the antibiotic thiostrepton), such an effect can be demonstrated directly. These conclusions imply a fundamental role for RNA in ribosomal function.

摘要

核糖体是一种酶,而酶具有活性位点。影响核糖体功能的抗生素可被视为酶抑制剂(或调节剂),因此,将其分子靶点作为研究该颗粒活性位点的一种手段是恰当的。本文考虑了用于此目的的现有方法,并对数据进行了总体评估。得出的结论是,几乎没有令人信服的证据表明抗生素主要与核糖体蛋白结合。相反,对各种系统中抗生素抗性的研究强烈表明,核糖体RNA是许多药物的主要靶点。此外,至少在一个案例中(与抗生素硫链丝菌素有关),这种作用可以直接得到证明。这些结论暗示了RNA在核糖体功能中具有重要作用。

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