Abstract
For monitoring low-density lipoprotein receptors (LDLr) in tumors and in livers of patients with familial hypercholesterolemia (FH) treated with gene therapy, a series of tricarbocyanine cholesteryl laurates were synthesized with the cholesteryl laurate moiety serving as the lipid-chelating anchor for low-density lipoprotein (LDL). One of these conjugates, TCL17, was successfully used to label LDL to give a new NIRF, TCL17-LDL. Ex vivo biological studies on an LDLr overexpressing tumor model, human hepatoblastoma G(2) (HepG(2)), confirmed that this NIRF were internalized selectively by the tumor and detected with high sensitivity by a low-temperature 3-D redox scanner.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Carbocyanines / chemical synthesis
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Carbocyanines / chemistry
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Carbocyanines / pharmacokinetics
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Cholesterol Esters / chemistry
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Cholesterol Esters / metabolism*
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Cholesterol Esters / pharmacokinetics
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Cholesterol, LDL / chemical synthesis
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Cholesterol, LDL / chemistry
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Cholesterol, LDL / metabolism*
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Cholesterol, LDL / pharmacokinetics
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Fluorescent Dyes / chemical synthesis
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Fluorescent Dyes / chemistry
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Fluorescent Dyes / metabolism*
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Fluorescent Dyes / pharmacokinetics
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Genetic Therapy
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Hepatoblastoma / drug therapy
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Hepatoblastoma / metabolism*
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Humans
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Hyperlipoproteinemia Type II / metabolism*
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Hyperlipoproteinemia Type II / therapy
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Imaging, Three-Dimensional
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Laurates / chemical synthesis
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Laurates / chemistry
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Laurates / metabolism*
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Laurates / pharmacokinetics
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Liver Neoplasms / metabolism*
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Liver Neoplasms / therapy
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Mice
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Receptors, LDL / metabolism*
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Spectroscopy, Near-Infrared
Substances
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Carbocyanines
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Cholesterol Esters
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Cholesterol, LDL
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Fluorescent Dyes
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Laurates
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Receptors, LDL