Tricarbocyanine cholesteryl laurates labeled LDL: new near infrared fluorescent probes (NIRFs) for monitoring tumors and gene therapy of familial hypercholesterolemia.

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.

• Authors: Gang Zheng, Hui Li, Kathy Yang, Dana Blessington, Kai Licha, Sissel Lund-Katz, Britton Chance, Jerry D Glickson
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 12 Issue 11 Pg. 1485-8 (Jun 03 2002) ISSN: 0960-894X [Print] England
• PMID: 12031325 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Carbocyanines
• Cholesterol Esters
• Cholesterol, LDL
• Fluorescent Dyes
• Laurates
• Receptors, LDL

Topics

• Animals
• Carbocyanines (chemical synthesis, chemistry, pharmacokinetics)
• Cholesterol Esters (chemistry, metabolism, pharmacokinetics)
• Cholesterol, LDL (chemical synthesis, chemistry, metabolism, pharmacokinetics)
• Fluorescent Dyes (chemical synthesis, chemistry, metabolism, pharmacokinetics)
• Genetic Therapy
• Hepatoblastoma (drug therapy, metabolism)
• Humans
• Hyperlipoproteinemia Type II (metabolism, therapy)
• Imaging, Three-Dimensional
• Laurates (chemical synthesis, chemistry, metabolism, pharmacokinetics)
• Liver Neoplasms (metabolism, therapy)
• Mice
• Receptors, LDL (metabolism)
• Spectroscopy, Near-Infrared