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Issue 6, 2012
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Cellular uptake of an α-AApeptide

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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.

Graphical abstract: Cellular uptake of an α-AApeptide

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The article was received on 03 Oct 2011, accepted on 29 Nov 2011 and first published on 30 Nov 2011

Article type: Communication
DOI: 10.1039/C2OB06679C
Citation: Org. Biomol. Chem., 2012,10, 1149-1153
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    Cellular uptake of an α-AApeptide

    G. Bai, S. Padhee, Y. Niu, R. E. Wang, Q. Qiao, R. Buzzeo, C. Cao and J. Cai, Org. Biomol. Chem., 2012, 10, 1149
    DOI: 10.1039/C2OB06679C

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