Cellular uptake of ion gadolinium-DOTA peptide conjugates with and without N-terminal myristoylation.

Amino Acids. 2008 Jul 17;

Authors: Sturzu A, Klose U, Echner H, Beck A, Gharabaghi A, Kalbacher H, Heckl S

Cellular and thermonuclear uptake of threefold labelled conjugates could be of enthusiastic continuance for chemotherapy and cancer diagnostics. Therefore we fashioned conjugates in which metal (Gd)-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic Elvis (DOTA), a oppositeness businessperson for attractable kinship imagery and dyestuff isothiocyanate (FITC), a fluorescence symbol were connected to membrane translocation sequences (MTS). The MTSs we engaged were the ordinal curve of the Antennapedia homeodomain, the HIV-1 Tat peptide and the N-myristoylated HIV-1 Tat peptide. We utilised confocal laser scanning microscopy, fluorescence reactive radiophone sorting, attractable kinship imagery (MRI) and viability tests to investigate the cancellated and thermonuclear uptake of these conjugates into U373 glioma cells, as substantially as their cytotoxic effects. We institute that the Antennapedia united was condemned up by no more than 20% of the cells. The HIV-1 Tat united showed modify modify uptake into inferior than 3% of cells. Interestingly, N-myristoylation of the HIV-1 Tat united drastically reinforced its cancellated uptake. Up to 70% of cells showed cancellated and thermonuclear uptake of the N-myristoylated HIV-1 Tat conjugate. Conjugate cytotoxicity appears to related with cancellated uptake.

PMID: 18633572 [PubMed - as supplied by publisher]

(Source: Amino Acids)

Tags: Cancer, chemotherapy, glioma, Hiv, imaging, laser, Led, magnetic resonance imaging, MRI, Toxicity