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Dendritic oligoguanidines as intracellular translocators
Author(s) -
Chung HyunHo,
Harms Guido,
Min Seong Churl,
Choi Byung Hyune,
Min Changhee,
Taulane Joseph P.,
Goodman Murray
Publication year - 2004
Publication title -
peptide science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.556
H-Index - 125
eISSN - 1097-0282
pISSN - 0006-3525
DOI - 10.1002/bip.10597
Subject(s) - chemistry , dendrimer , intracellular , green fluorescent protein , fluorescein , hela , biophysics , microbiology and biotechnology , dendritic cell , fluorescence , cell , biochemistry , biology , antigen , gene , physics , genetics , quantum mechanics
A series of polyguanidylated dendritic structures that can be used as molecular translocators have been designed and synthesized based on nonpeptide units. The dendritic oligoguanidines conjugated with fluorescein or with a green fluorescent protein (GFP) mutant as cargos were isolated and characterized. Quantification and time‐course analyses of the cellular uptake of the conjugates using HeLa S3 and human cervical carcinoma cells reveal that the polyguanidylated dendrimers have comparable translocation efficiency to the Tat (49–57) peptide. Furthermore, the deconvolution microscopy image analysis shows that they are located inside the cells. These results clearly show that nonlinear, branched dendritic oligoguanidines are capable of translocation through the cell membrane. This work also demonstrates the potential of these nonpeptidic dendritic oligoguanidines as carriers for intracellular delivery of small molecule drugs, bioactive peptides, and proteins. © 2004 Wiley Periodicals, Inc. Biopolymers (Pept Sci), 2004