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Cellular uptake of an α-AApeptide.
- Source :
-
Organic & biomolecular chemistry [Org Biomol Chem] 2012 Feb 14; Vol. 10 (6), pp. 1149-53. Date of Electronic Publication: 2011 Dec 23. - Publication Year :
- 2012
-
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.
- Subjects :
- Cell Survival drug effects
Cytoplasm metabolism
Dose-Response Relationship, Drug
Endosomes metabolism
Gene Products, tat chemistry
Gene Products, tat metabolism
HeLa Cells
Humans
Jurkat Cells
Molecular Conformation
Peptides chemical synthesis
Peptides pharmacology
Stereoisomerism
Structure-Activity Relationship
Peptides chemistry
Peptides metabolism
Permeability drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 1477-0539
- Volume :
- 10
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- Organic & biomolecular chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 22193209
- Full Text :
- https://doi.org/10.1039/c2ob06679c