Macrocyclic Chelators with Paramagnetic Cations Are Internalized into Mammalian Cells via a HIV-Tat Derived Membrane Translocation Peptide

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 c...

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Veröffentlicht in:Bioconjugate chemistry 2000-05, Vol.11 (3), p.301-305
Hauptverfasser: Bhorade, Rajeev, Weissleder, Ralph, Nakakoshi, Tsunenori, Moore, Anna, Tung, Ching-Hsuan
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container_end_page 305
container_issue 3
container_start_page 301
container_title Bioconjugate chemistry
container_volume 11
creator Bhorade, Rajeev
Weissleder, Ralph
Nakakoshi, Tsunenori
Moore, Anna
Tung, Ching-Hsuan
description 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.
doi_str_mv 10.1021/bc990168d
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source MEDLINE; American Chemical Society Journals
subjects AIDS/HIV
Amino Acid Sequence
Animals
Biological Transport
Cell Membrane - metabolism
Cell Nucleus - metabolism
Chelating Agents - metabolism
Cytoplasm - metabolism
Dysprosium
Gadolinium
Gene Products, tat - chemical synthesis
Gene Products, tat - chemistry
Gene Products, tat - metabolism
HeLa Cells
Heterocyclic Compounds, 1-Ring - chemical synthesis
Heterocyclic Compounds, 1-Ring - chemistry
Heterocyclic Compounds, 1-Ring - metabolism
Humans
Indium Radioisotopes
Lymphocytes - metabolism
Lymphocytes - ultrastructure
Magnetic Resonance Imaging
Mice
Molecular Sequence Data
Peptide Fragments - chemistry
Peptide Fragments - metabolism
tat Gene Products, Human Immunodeficiency Virus
title Macrocyclic Chelators with Paramagnetic Cations Are Internalized into Mammalian Cells via a HIV-Tat Derived Membrane Translocation Peptide
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