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一种由13个氨基酸残基组成的抗菌溶血肽中谷氨酸突变为赖氨酸,可增强抗菌活性且不增加溶血活性。

Change of glutamic acid to lysine in a 13-residue antibacterial and hemolytic peptide results in enhanced antibacterial activity without increase in hemolytic activity.

作者信息

Sitaram N, Chandy M, Pillai V N, Nagaraj R

机构信息

Centre for Cellular and Molecular Biology, Hyderabad, India.

出版信息

Antimicrob Agents Chemother. 1992 Nov;36(11):2468-72. doi: 10.1128/AAC.36.11.2468.

Abstract

A 13-residue peptide corresponding to a hydrophobic segment of the antimicrobial 47-residue peptide seminalplasmin, PKLLETFLSKWIG (SPF), has been shown to have antibacterial and hemolytic activities (N. Sitaram and R. Nagaraj, J. Biol. Chem. 265:10438-10442, 1990). In an effort to get an insight into the structural and charge requirements for these biological activities, an analog of SPF in which Glu has been replaced with Lys has been synthesized and its antibacterial and hemolytic properties have been examined. It has been demonstrated that the analog, SPFK, exhibits potent antibacterial activity at concentrations at which hemolysis does not occur.

摘要

一种由13个氨基酸残基组成的肽,对应于抗菌性47个氨基酸残基的肽精浆蛋白(PKLLETFLSKWIG,简称SPF)的疏水片段,已被证明具有抗菌和溶血活性(N. 西塔拉姆和R. 纳加拉吉,《生物化学杂志》265:10438 - 10442,1990年)。为了深入了解这些生物活性的结构和电荷要求,合成了一种SPF类似物,其中谷氨酸被赖氨酸取代,并检测了其抗菌和溶血特性。已经证明,该类似物SPFK在不发生溶血的浓度下表现出强大的抗菌活性。

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Synthetic magainin analogues with improved antimicrobial activity.
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