Novel and Selective Fluorescent σ2-Receptor Ligand with a 3,4-Dihydroisoquinolin-1-one Scaffold: A Tool to Study σ2Receptors in Living Cells
| Autor: | Francesco Berardi, Dario Ghigo, Maria Laura Pati, Mauro Niso, Chiara Riganti, Carmen Abate |
|---|---|
| Rok vydání: | 2015 |
| Předmět: |
ligand design
Scaffold Cell Survival Biology Biochemistry Substrate Specificity Flow cytometry Western blot fluorescent probes medicine Humans Receptors sigma cancer Fluorescent tracer Receptor Molecular Biology Fluorescent Dyes medicine.diagnostic_test flow cytometry Organic Chemistry Isoquinolines Ligand (biochemistry) Fluorescence Molecular biology sigma receptors Cell culture Drug Design Molecular Medicine Protein Binding |
| Zdroj: | ChemBioChem. 16:1078-1083 |
| ISSN: | 1439-4227 |
| Popis: | Although sigma-2 (σ2 ) receptors are still enigmatic proteins, they are promising targets for tumor treatment and diagnosis. With the aim of clarifying their role in oncology, we developed a σ2 -selective fluorescent tracer (compound 5) as a specific tool to study σ2 receptors. By using flow cytometry with 5, we performed competition binding studies on three different cell lines where we also detected the content of the σ2 receptors, avoiding the inconvenient use of radioligands. Comparison with a previously developed mixed σ1 /σ2 fluorescent tracer (1) also allowed for the detection of σ1 receptors within these cells. Results obtained by flow cytometry with tracers 1 and 5 were confirmed by standard methods (western blot for σ1 , and Scatchard analysis for σ2 receptors). Thus, we have produced powerful new tools for research on the σ whose reliability and adaptability to a number of fluorescence techniques will be useful to elucidate the roles of σ receptors in oncology. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Plný text