摘要:
AbstractTwo types of cationic cyclic α,α‐disubstituted α‐amino acids: Api
(which possesses a lysine mimic side chain) and ApiC2Gu (which possesses an arginine mimic side chain), were developed. These amino acids were incorporated into an arginine‐based peptide sequence [(l‐Arg‐l‐Arg‐dAA)3: dAA=Api
or ApiC2Gu], and the relationship between the secondary structures of the resulting peptides and their ability to pass through cell membranes was investigated. The peptide containing ApiC2Gu formed a stable α‐helical structure and was more effective at penetrating cells than the nonhelical Arg nonapeptide (R9). Furthermore, the peptide was able to deliver plasmid DNA into various types of cells in a highly efficient manner.