title: Cellular uptake of an α-AApeptide.
abstract: Some short and cationic peptides such as the Tat peptide can cross the cell membrane and function as vectors for intracellular delivery. Here we show that an α-AApeptide is able to penetrate the membranes of living cells from an extracellular environment and enter the endosome and cytoplasm of cells. The efficiency of the cellular uptake is comparable to a Tat peptide (48-57) of the same length and is unexpectedly superior to an α-peptide with identical functional groups. The mechanism of uptake is similar to that of the Tat peptide and is through endocytosis by an energy-dependent pathway. Due to the easy synthesis of the α-AApeptides, their resistance to proteolytic hydrolysis, and their low cytotoxicity, α-AApeptides represent a new class of transporters for the delivery of drugs.
authors.affiliation: Department of Chemistry, University of South Florida, 4202 E. Fowler Ave, Tampa, FL 33620, USA.
authors.forename: Ge
authors.initials: G
authors.lastname: Bai
authors.forename: Shruti
authors.initials: S
authors.lastname: Padhee
authors.forename: Youhong
authors.initials: Y
authors.lastname: Niu
authors.forename: Rongsheng E
authors.initials: RE
authors.lastname: Wang
authors.forename: Qiao
authors.initials: Q
authors.lastname: Qiao
authors.forename: Robert
authors.initials: R
authors.lastname: Buzzeo
authors.forename: Chuanhai
authors.initials: C
authors.lastname: Cao
authors.forename: Jianfeng
authors.initials: J
authors.lastname: Cai
mesh_terms: D002470:Cell Survival / Q000187:drug effects; D003593:Cytoplasm / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D011992:Endosomes / Q000378:metabolism; D015696:Gene Products, tat / Q000737:chemistry / Q000378:metabolism; D006367:HeLa Cells; D006801:Humans; D019169:Jurkat Cells; D008968:Molecular Conformation; D010455:Peptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism* / Q000494:pharmacology; D010539:Permeability / Q000187:drug effects; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D015696:Gene Products, tat; D010455:Peptides