Abstract
Gene therapy has emerged as a promising strategy for treatment of various diseases, but there is a pressing need for the development of non-invasive reporter techniques based on appropriate molecules and imaging modalities to assay gene expression. We now report the design, synthesis, and evaluation of novel enhanced reporter molecules, which reveal lacZ gene expression: trifluoromethylated aryl β-d-galactopyranosides. A series of five molecular structures were screened in solution and with stably transfected lacZ expressing human MCF7 breast cancer cells in vitro. p-Trifluoromethyl-o- nitrophenyl β-d-galactopyranoside (PCF3ONPG) was found to exhibit valuable properties including a single 19F NMR signal, stability in aqueous solution and with wild type cells, but a chemical shift response to enzyme cleavage (Δδ = 1.14 ppm) in breast cancer cells transfected to stably express lacZ.
Original language | English (US) |
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Pages (from-to) | 326-333 |
Number of pages | 8 |
Journal | Bioorganic and Medicinal Chemistry |
Volume | 14 |
Issue number | 2 |
DOIs | |
State | Published - Jan 15 2006 |
Keywords
- F NMR
- Reporter gene
- lacZ
- β-Galactosidase
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry