A novel conjugable translocator protein ligand labeled with a fluorescence dye for in vitro imaging.

Bai M, Wyatt SK, Han Z, Papadopoulos V, Bornhop DJ
Bioconjug Chem. 2007 18 (4): 1118-22

PMID: 17552492 · DOI:10.1021/bc060381r

A conjugable analogue of the benzodiazepine 4' '-chlorodiazepam (Ro5-4864), C6Ro5-4864 was synthesized to probe the binding sites of translocator protein (18 kDa; TSPO), previously known as the peripheral benzodiazepine receptor for molecular imaging. The amino group in this analogue allows universal conjugation to signaling molecules. Lissamine-C6Ro5-4864, synthesized from C6Ro5-4864 and a lissamine fluorescence dye, was investigated in this study. This imaging agent exhibited micromolar binding affinity (Ki = 2.6 microM) to TSPO and was successfully imaged in TSPO rich glioma and breast cancer cell lines. These findings suggest that C6Ro5-4864 may provide opportunities in imaging disease states where TSPO levels are affected, such as cancer and neurologic diseases.

MeSH Terms (11)

Animals Benzodiazepinones Cell Line, Tumor Fluorescent Dyes Humans Ligands Microscopy, Fluorescence Protein Binding Rats Receptors, GABA Rhodamines

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