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

TitleMacrocyclic chelators with paramagnetic cations are internalized into mammalian cells via a HIV-tat derived membrane translocation peptide.
Publication TypeJournal Article
Year of Publication2000
AuthorsBhorade R, Weissleder R, Nakakoshi T, Moore A, Tung CH
JournalBioconjug Chem
Volume11
Issue3
Pagination301-5
Date Published2000 May-Jun
ISSN1043-1802
KeywordsAmino Acid Sequence, Animals, Biological Transport, Cell Membrane, Cell Nucleus, Chelating Agents, Cytoplasm, Dysprosium, Gadolinium, Gene Products, tat, HeLa Cells, Heterocyclic Compounds, 1-Ring, Humans, Indium Radioisotopes, Lymphocytes, Magnetic Resonance Imaging, Mice, Molecular Sequence Data, Peptide Fragments, tat Gene Products, Human Immunodeficiency Virus
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.

DOI10.1021/bc990168d
Alternate JournalBioconjug Chem
PubMed ID10821645
Grant ListR01AI-CA46973 / AI / NIAID NIH HHS / United States
R21DK55713 / DK / NIDDK NIH HHS / United States
Related Institute: 
Molecular Imaging Innovations Institute (MI3)

Weill Cornell Medicine
Department of Radiology
525 East 68th Street New York, NY 10065