...
首页> 外文期刊>Biochemistry >Studies on amino acid replacement and inhibitory activity of a [beta]-lactamase inhibitory peptide
【24h】

Studies on amino acid replacement and inhibitory activity of a [beta]-lactamase inhibitory peptide

机译:β-内酰胺酶抑制肽的氨基酸置换和抑制活性的研究

获取原文
获取原文并翻译 | 示例
           

摘要

An SHV β-lactamase gene was amplified from a β-lactam resistant Klebsiella pneumoniae K-71 genomic DNA. After expression and purification, we demonstrated that peptide P1 could inhibit the hydrolysis activity of both TEM-1 and SHV β-lactamase in vitro. Three mutations were introduced into P1 in which the first residue S was replaced by F, the 18th residue V was mutated to Y, and the 15th residue Y was substituted with A, C, G, and R to obtain the mutants of P1-A, P1- C, P1-G, and P1-R, respectively. The mutant peptides were purified and their inhibitory constants against TEM-1 and SHV β-lactamase were determined. All these β-lactamase inhibitory peptides could inhibit the activity of both β-lactamases, while the mutant peptides showed stronger inhibitory activities against TEM-1 β-lactamase than against SHV β-lactamase. Inhibition data suggested that P1-A improved the β-lactamase inhibitory activity by over 3-fold compare to P1. When P1-A was incubated with K. pneumoniae K-71 in Luria-Bertani medium containing ampicillin, it showed a much stronger growth of inhibition ratio over P1. This study gives us a good candidate for development of novel β-lactamase inhibitors.[PUBLICATION ABSTRACT]
机译:从抗β-内酰胺的肺炎克雷伯菌K-71基因组DNA中扩增出SHVβ-内酰胺酶基因。经过表达和纯化,我们证明了肽P1可以在体外抑制TEM-1和SHVβ-内酰胺酶的水解活性。将三个突变引入P1,其中第一个残基S被F取代,第18个残基V被突变为Y,第15个残基Y被A,C,G和R取代,从而获得P1-A的突变体,P1-C,P1-G和P1-R。纯化突变肽,并测定其对TEM-1和SHVβ-内酰胺酶的抑制常数。所有这些β-内酰胺酶抑制肽都能抑制两种β-内酰胺酶的活性,而突变肽对TEM-1β-内酰胺酶的抑制活性比对SHVβ-内酰胺酶的抑制活性强。抑制数据表明,与P1相比,P1-A将β-内酰胺酶的抑制活性提高了3倍以上。当将P1-A与肺炎克雷伯氏菌K-71在含有氨苄青霉素的Luria-Bertani培养基中孵育时,其抑制率的增长远高于P1。这项研究为我们开发新型β-内酰胺酶抑制剂提供了一个很好的候选者。[出版物摘要]

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号