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Phenylboronate 160Tb complexes for molecular recognition of glycoproteins expressed on tumor cells.

Abstract：

:The over-expression of sialic acid on the surface of cancer cells compared with normal ones makes this nine-carbon sugar an attractive biomarker for molecular diagnosis and therapy. Here, we describe a study on the molecular recognition of sialic acid end groups on the surface of human glioma cells by (160)Tb-DTPA-EN(2), (160)Tb-DTPA-(ENPBA)(2) and (160)Tb-DTPA-(PBA)(2) complexes. The results show Tb-DTPA-(ENPBA)(2) to be the most efficient targeting agent, due to the electrostatic interaction between its two positively charged ammonium groups and the negatively charged cell surface, which provides an additional stabilization of the covalent binding through the PBA moieties and the sialic acid diol functions. Up to 5.5 nmol Tb/mg protein is taken up by the cells. ICP analysis after incubation experiments with non-radioactive Tb-DTPA-(ENPBA)(2) suggests that dissociation of Tb from this complex occurs after its binding to the cell surface. Most likely, most of the free Tb remains adsorbed on the surface of the cells, although internalization of a small amount cannot be excluded.

journal_name

Contrast Media Mol Imaging

journal_title

Contrast media & molecular imaging

authors

Djanashvili K,Koning GA,van der Meer AJ,Wolterbeek HT,Peters JA

doi

10.1002/cmmi.123

subject

Has Abstract

pub_date

2007-01-01 00:00:00

pages

35-41

issue

1

eissn

1555-4309

issn

1555-4317

journal_volume

2

pub_type

杂志文章

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