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Specific labeling with potent radiolabels alters the uptake of cell‐penetrating peptides
Author(s) -
Walther Cornelia,
Ott Ingo,
Gust Ronald,
Neundorf Ines
Publication year - 2009
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.21218
Subject(s) - internalization , chemistry , cell penetrating peptide , peptide , hela , radionuclide therapy , dota , oligopeptide , biophysics , nanotechnology , computational biology , cell , combinatorial chemistry , biochemistry , chelation , medicine , materials science , organic chemistry , biology , nuclear medicine
Radiolabeled peptides play an important role in radiopharmacy not only as tumor markers but also as transport vectors. Therefore, cell‐penetrating peptides (CPP) may serve as very effective delivery tools, as well. Recently, CPP based on the human hormone calcitonin (hCT) have been developed. Especially, branched hCT‐peptide sequences turned out to have highly efficient internalization capacities. Labeling these peptides with radionuclides would generate promising new tools for imaging and therapy applications in radiopharmacy. However, the influence of the metal complexation on the internalization capacity of CPP has not been elucidated yet in detail. In this study we quantified the uptake of Ga‐DOTA modified hCT‐carrier peptides in HeLa cells by using atomic absorption spectroscopy (AAS) and compared the results to the uptake of fluorescently‐labeled peptides. Interestingly, we measured different uptake rates depending on the attached label. Unexpectedly, modification with a Ga‐DOTA complex can have tremendous effects on the uptake efficiency. The results of these studies support the need of detailed analysis of each carrier peptide/cargo construct, especially in the field of metal complex modified CPP. © 2009 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 92: 445–451, 2009. This article was originally published online as an accepted preprint. The “Published Online” date corresponds to the preprint version. You can request a copy of the preprint by emailing the Biopolymers editorial office at biopolymers@wiley.com