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Alanine and Lysine Scans of the LL‐37‐Derived Peptide Fragment KR‐12 Reveal Key Residues for Antimicrobial Activity
ChemBioChem ( IF 3.2 ) Pub Date : 2018-03-30 , DOI: 10.1002/cbic.201700599
Sunithi Gunasekera 1 , Taj Muhammad 1 , Adam A. Strömstedt 1 , K. Johan Rosengren 2 , Ulf Göransson 1
Affiliation  

Pinpointing critical positions: Alanine and lysine scans demonstrate that substituting amino acids 5 and 9 increases the activity of KR‐12 against human pathogens. Cationic substitutions in other positions lead to changes in specificity. Membrane‐permeabilisation assays show the same trends, which indicate membrane disruption as a mechanism of action, but peptides show no cytotoxic activity against human cells.
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中文翻译:

LL 37衍生肽片段KR-12的丙氨酸和赖氨酸扫描揭示了抗菌活性的关键残基

查明关键位置:丙氨酸和赖氨酸扫描表明,用氨基酸5和9取代可增加KR-12抵抗人类病原体的活性。其他位置的阳离子取代会导致特异性变化。膜通透性测定显示出相同的趋势,表明膜破坏是一种作用机制,但是肽对人细胞没有细胞毒性。
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更新日期:2018-03-30
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