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亚砜部分对稀疏霉素类似物生化及生物学特性的必要性

Necessity of the sulfoxide moiety for the biochemical and biological properties of an analog of sparsomycin.

作者信息

Flynn G A, Ash R J

出版信息

Biochem Biophys Res Commun. 1983 Jul 18;114(1):1-7. doi: 10.1016/0006-291x(83)91585-1.

DOI:10.1016/0006-291x(83)91585-1
PMID:6349625
Abstract

An analog of the peptidyl transferase inhibitor sparsomycin was a competitive inhibitor (Ki = 1.8 microM) of peptidyl-puromycin synthesis on E. coli polysomes. Preincubation of polysomes with the compound enhanced the degree of inhibition of peptide bond formation. A model for the involvement of a histidine residue in peptidyl transferase activity is presented as a result of our observations which include direct association of [3H] labelled analog with 70S ribosomes. The correct oxidation state of sulfur in the compound was necessary for the "preincubation effect" and entry of the compound into bacterial cells.

摘要

肽基转移酶抑制剂稀疏霉素的一种类似物是大肠杆菌多核糖体上肽基嘌呤霉素合成的竞争性抑制剂（Ki = 1.8 microM）。多核糖体与该化合物预孵育可增强肽键形成的抑制程度。基于我们的观察结果提出了一种组氨酸残基参与肽基转移酶活性的模型，这些观察结果包括[3H]标记的类似物与70S核糖体的直接结合。化合物中硫的正确氧化态对于“预孵育效应”以及化合物进入细菌细胞是必需的。

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1
Necessity of the sulfoxide moiety for the biochemical and biological properties of an analog of sparsomycin.亚砜部分对稀疏霉素类似物生化及生物学特性的必要性
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Effect of sparsomycin analogues on the puromycin-peptidyl transferase reaction on ribosomes.稀疏霉素类似物对核糖体上嘌呤霉素 - 肽基转移酶反应的影响。
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Sulfoxide configuration in sparsomycin determines time-dependent and competitive inhibition of peptidyl transferase.稀疏霉素中的亚砜构型决定了肽基转移酶的时间依赖性和竞争性抑制作用。
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引用本文的文献

1
Importance of the hydrophobic sulfoxide substituent on nontoxic analogs of sparsomycin.疏水亚砜取代基对稀疏霉素无毒类似物的重要性。
Antimicrob Agents Chemother. 1984 Apr;25(4):443-5. doi: 10.1128/AAC.25.4.443.
2
Interaction of the antibiotic sparsomycin with the ribosome.抗生素 sparsomycin 与核糖体的相互作用。
Antimicrob Agents Chemother. 1991 Jan;35(1):10-3. doi: 10.1128/AAC.35.1.10.

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