A Novel Conjugable Translocator Protein Ligand Labeled with a Fluorescence Dye for in Vitro Imaging

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 universa...

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Bibliographic Details
Published in:Bioconjugate chemistry 2007-07, Vol.18 (4), p.1118-1122
Main Authors: Bai, Mingfeng, Wyatt, Shelby K, Han, Zeqiu, Papadopoulos, Vassilios, Bornhop, Darryl J
Format: Article
Language:English
Subjects:
Amino acids
Animals
Benzodiazepinones - chemistry
Benzodiazepinones - metabolism
Biochemistry
Cell Line, Tumor
Dyes
Fluorescent Dyes - chemistry
Fluorescent Dyes - metabolism
Humans
Ligands
Medical imaging
Microscopy, Fluorescence
Molecules
Protein Binding
Proteins
Rats
Receptors, GABA - chemistry
Receptors, GABA - metabolism
Rhodamines - chemistry
Rhodamines - metabolism
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Summary: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 (K i = 2.6 μM) 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.
ISSN:1043-1802
1520-4812
DOI:10.1021/bc060381r