“Minimalist” antimicrobial peptides are disclosed based on 50 to 80% &agr;,&agr;-dialkylated amino acids. The peptides are short, cationic, amphipathic, and possess a high helix propensity. Polar &agr;,&agr;-dialkylated amino acids are also disclosed. These peptides are easy and inexpensive to synthesize via solid-phase techniques. The peptides exhibit in vitro anti-bacterial properties at concentrations that are not lethal to normal mammalian cells. The peptides exhibit in vivo bioactivity against intracellular pathogens.
已公开的 "极简 "抗菌肽基于 50% 至 80% 的二烷基化
氨基酸。这些肽是短的、阳离子的、两性的,并具有较高的螺旋倾向。还公开了极性二烷基化
氨基酸。这些肽易于通过固相技术合成,成本低廉。这些肽在体外表现出抗菌特性,其浓度对正常哺乳动物细胞无致命影响。这些肽在体内对细胞内病原体具有
生物活性。