Macrocyclic chelators with paramagnetic cations are internalized into mammalian cells via a HIV-tat derived membrane translocation peptide.

Important note: Information in this article was accurate in 2000. The state of the art may have changed since the publication date.

Macrocyclic chelators with paramagnetic cations are internalized into mammalian cells via a HIV-tat derived membrane translocation peptide.

Bioconjug Chem. 2000 May-Jun;11(3):301-5. Unique Identifier : AIDSLINE MED/20281353
Bhorade R; Weissleder R; Nakakoshi T; Moore A; Tung CH; Center for Molecular Imaging Research, Massachusetts General; Hospital, Harvard Medical School, 149 13th St., #5406,; Charlestown, Massachusetts 02129, USA.

Abstract: A major obstacle to using paramagnetic MR contrast agents for in vivo cell tracking or molecular sensing is their generally low cellular uptake. In this study, we show that a paramagnetically labeled DOTA chelator derivatized with a 13-mer HIV-tat peptide is efficiently internalized into mammalian cells. Intracellular concentrations were attained that were readily detectable by MR imaging using both gadolinium and dysprosium chelates. Using this paradigm, it should be feasible to internalize a variety of chemically different agents into mammalian cells.

Keywords: JOURNAL ARTICLE Amino Acid Sequence Animal Biological Transport Cell Membrane/METABOLISM Cell Nucleus/METABOLISM Chelating Agents/*METABOLISM Cytoplasm/METABOLISM Dysprosium Gadolinium Gene Products, tat/CHEMISTRY/CHEMICAL SYNTHESIS/*METABOLISM Hela Cells Heterocyclic Compounds, 1-Ring/CHEMISTRY/CHEMICAL SYNTHESIS/ *METABOLISM Human Indium Radioisotopes Lymphocytes/METABOLISM/ULTRASTRUCTURE *Magnetic Resonance Imaging Mice Molecular Sequence Data Peptide Fragments/CHEMISTRY/*METABOLISM Support, U.S. Gov't, P.H.S.
001030
A00A1136

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