Abstract
Peptaibols are a large family of linear, amphipathic polypeptides consisting of 5-20 amino acid residues generated from the fungal nonribosomal peptide synthetase (NRPS) pathway. With a relatively high content of non-proteinogenic amino acids such as α-aminoisobutyrate (Aib) and isovaline (Iva) in the skeleton, peptaibols exhibit a wide range of biological activities, including anti-microbial, cytotoxic, and neuroleptic effects. With five peptaibols brought to market for use as biocontrol agents, this class of peptides has received increasing attention from both biochemists and pharmacologists. In this review, we summarized the progress made in structural characterization, elucidation of biosynthetic pathways, and investigation of biosynthesis elucidation and bioactivities, to promote further efforts to develop peptaibols as pharmaceuticals.