期刊
FEBS LETTERS
卷 580, 期 5, 页码 1451-1456出版社
WILEY
DOI: 10.1016/j.febslet.2006.01.077
关键词
cell penetrating peptide; peptide nucleic acid; photochemical internalization; antisense; luciferase
Recent studies have shown that endosomal release is a major rate-limiting step for cellular delivery via a variety of cationic cell penetrating peptides. Thus, methods and/or protocols for effective release of endosomally entrapped drugs are highly warranted. Photochemical internalization (PCI) has previously been proposed for this purpose. Here, we demonstrate an enhancement of up to two orders of magnitude of the antisense effects (cytosolic/nuclear) of peptide nucleic acid-peptide conjugates (Tat, Arg(7), KLA) in HeLa cells by a PCI approach using the photosensitizer AIPc(2)a. These results emphasize the importance of endosomal release for cellular activity of this type of drug delivery and also raise hope that methods like PCI which have applications for in vivo use may also enhance the bioavailability and in vivo efficacy of these types of conjugates. (c) 2006 Federation of European Biochemical Societies. Published by Elsevier B.V. All rights reserved.
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