Novel and Selective Fluorescent σ2‐Receptor Ligand with a 3,4‐Dihydroisoquinolin‐1‐one Scaffold: A Tool to Study σ2 Receptors in Living Cells |
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Authors: | Dr. Mauro Niso Dr. Chiara Riganti Maria Laura Pati Prof. Dario Ghigo Prof. Francesco Berardi Carmen Abate |
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Affiliation: | 1. Dipartimento di Farmacia‐Scienze del Farmaco, Via Orabona, 4. 70125 Bari (Italy);2. Department of Oncology, University of Turin via Santena 5/bis, 10126, Torino (Italy) |
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Abstract: | 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. |
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Keywords: | cancer flow cytometry fluorescent probes ligand design sigma receptors |
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