19F-MRS/1H-MRI dual-function probe for detection of β-galactosidase activity?

Chemical Science Pub Date: 2013-02-25 DOI: 10.1039/C3SC21099E

Abstract

Because of the importance of lacZ gene in various applications ranging from molecular biology to clinical trials, the development of non-invasive bimodal techniques for improving precision and accuracy to assay gene expression has attracted much attention. In this paper, we propose a dual-function probe for synergistic combination of 19F-MRS/1H-MRI to simultaneously detect β-gal activity. Based on this strategy, we have designed, synthesized and characterized a series of 19F-MRS/1H-MRI reporters, and demonstrated the feasibility of 1-O-(β-D-galactopyranosyl)-3-fluorocatechol MGD-3-FCAT for assessing β-gal activity in solution and in vitro with lacZ transfected tumor cells as well, by the characterization of β-gal responsive 19F-chemical shift changes ΔδF, hydrolytic kinetics, and T1, T2 relaxation mapping.

Graphical abstract: 19F-MRS/1H-MRI dual-function probe for detection of β-galactosidase activity
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