Receptor mediated uptake of a radiolabeled contrast agent sensitive to β-galactosidase activity

Mian M. Alauddin, Angelique Y. Louie, Antranik Shahinian, Thomas J. Meade, Peter S. Conti

Research output: Contribution to journalArticle

33 Scopus citations

Abstract

Radiolabeling of the MRI contrast agent 1-[2-(β-galactopyranosyloxy)propyl]-4,7,10- tris(carboxymethyl)-1,4,7,10-tetraazacyclododecane with 111In, and its evaluation is reported. Radiolabeling was performed in acetate buffer with 50-78% radiochemical yield. In vitro studies revealed that the asialoglycoprotein receptor-poor cell line MH1C1 has low uptake, while the receptor-rich cell lines BNL-CL2 and Hep G2 have higher uptake. In vivo, the uptake of the compound in receptor-rich organ liver was very high. Blocking the receptor in vivo, reduced liver uptake by 90% suggesting that the compound localizes in receptor-enriched tissues by binding to the asialoglycoprotein receptor.

Original languageEnglish (US)
Pages (from-to)261-265
Number of pages5
JournalNuclear Medicine and Biology
Volume30
Issue number3
DOIs
StatePublished - Apr 2003

Keywords

  • β-Gal
  • In
  • Asialoglycoprotein receptor
  • MRI contrast agent

ASJC Scopus subject areas

  • Cancer Research
  • Molecular Medicine
  • Radiology Nuclear Medicine and imaging

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