Division of Organic Chemistry, National Institute of Health Sciences, 3-25-26, Tonomachi, Kawasaki, Kanagawa, 210-9501, Japan.
Graduate School of Medical Life Science, Yokohama City University, 1-7-29, Yokohama, Kanagawa, 230-0045, Japan.
ChemMedChem. 2021 Apr 20;16(8):1226-1233. doi: 10.1002/cmdc.202000940. Epub 2021 Feb 10.
Antimicrobial peptides (AMPs) are potential novel therapeutic drugs against microbial infections. Most AMPs function by disrupting microbial membranes because of their amphipathic properties and ordered secondary structures. In this minireview, we describe recent efforts to develop helical AMP foldamers containing non-proteinogenic amino acids, such as α,α-disubstituted α-amino acids, β-amino acids, γ-amino acids, side-chain stapling and N-alkyl glycines.
抗菌肽 (AMPs) 是一种对抗微生物感染的新型潜在治疗药物。由于其两亲性特性和有序的二级结构,大多数 AMP 通过破坏微生物膜来发挥作用。在这篇综述中,我们描述了最近在开发含有非天然氨基酸的螺旋 AMP 折叠体方面的努力,例如 α,α-二取代的 α-氨基酸、β-氨基酸、γ-氨基酸、侧链固定和 N-烷基甘氨酸。