Institute of Biotechnology and Department of Medical Science, National Tsing Hua University, Hsinchu 300, Taiwan.
Antimicrob Agents Chemother. 2011 Oct;55(10):4918-21. doi: 10.1128/AAC.00202-11. Epub 2011 Jul 18.
The efficacies of many antimicrobial peptides are greatly reduced under high salt concentrations, limiting their development as pharmaceutical compounds. Here, we describe an easy strategy to increase salt resistance of antimicrobial peptides by replacing tryptophan or histidine residues with the bulky amino acids β-naphthylalanine and β-(4,4'-biphenyl)alanine. The activities of the salt-sensitive peptide P-113 were diminished at high salt concentrations, whereas the activities of its β-naphthylalanine and β-(4,4'-biphenyl)alanine-substituted variant were less affected.
许多抗菌肽在高盐浓度下的功效大大降低，限制了它们作为药物化合物的开发。在这里，我们描述了一种通过用大体积氨基酸β-萘丙氨酸和β-(4,4'-联苯)丙氨酸取代色氨酸或组氨酸残基来提高抗菌肽耐盐性的简单策略。盐敏感肽 P-113 的活性在高盐浓度下降低，而其β-萘丙氨酸和β-(4,4'-联苯)丙氨酸取代变体的活性受影响较小。
