Seeking to increase the selectivity of antimicrobial peptides for prokaryotic cells, we incorporated a bis-dipicolyl amine (bis-DPA) ligand at the N-terminus of de novo designed model peptides. The Zn₂·bisDPA complex increases the interaction of peptides with anionic model membranes, while decreasing interactions with zwitterionic model membranes. Further, it improves the peptides’ antimicrobial activity and decreases their hemolytic activity without substantial changes to their secondary structure. Therefore, incorporating a Zn₂·bisDPA complex is a useful strategy to enhance the selectivity of antimicrobial peptides.

中文翻译：

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通过Zn（II）络合调节膜活性肽的活性

为了增加抗微生物肽对原核细胞的选择性，我们在从头设计的模型肽的N-末端掺入了双-二甲基吡啶胺（bis-DPA）配体。Zn ₂ ·bisDPA复合物增加了肽与阴离子模型膜的相互作用，同时减少了与两性离子模型膜的相互作用。此外，它在不显着改变其二级结构的情况下改善了肽的抗微生物活性并降低了其溶血活性。因此，掺入Zn ₂ ·bisDPA复合物是提高抗菌肽选择性的有用策略。