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Si us plau utilitzeu sempre aquest identificador per citar o enllaçar aquest document: https://hdl.handle.net/2445/200655
Development of a novel 1 receptor biosensor based on its heterodimerization with binding immunoglobulin protein in living cells
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The σ1 receptor (S1R) is a ligand-regulated non-opioid intracellular receptor involved in several pathological conditions. The development of S1R-based drugs as therapeutic agents is a challenge due to the lack of simple functional assays to identify and classify S1R ligands. We have developed a novel nanoluciferase binary technology (NanoBiT) assay based on the ability of S1R to heteromerize with the binding immunoglobulin protein (BiP) in living cells. The S1R-BiP heterodimerization biosensor allows for rapid and accurate identification of S1R ligands by monitoring the dynamics of association-dissociation of S1R and BiP. Acute treatment of cells with the S1R agonist PRE-084 produced rapid and transient dissociation of the S1R-BiP heterodimer, which was blocked by haloperidol. The effect of PRE-084 was enhanced by calcium depletion, leading to a higher reduction in heterodimerization even in the presence of haloperidol. Prolonged incubation of cells with S1R antagonists (haloperidol, NE-100, BD-1047, and PD-144418) increased the formation of S1R-BiP heteromers, while agonists (PRE-084, 4-IBP, and pentazocine) did not alter heterodimerization under the same experimental conditions. The newly developed S1R-BiP biosensor is a simple and effective tool for exploring S1R pharmacology in an easy cellular setting. This biosensor is suitable for high-throughput applications and a valuable resource in the researcher's toolkit.
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MORATÓ ARÚS, Xavier, FERNÁNDEZ DUEÑAS, Víctor, PÉREZ-VILLAMOR, Pilar, VALLE LEÓN, Marta, VELA, José miguel, MERLOS ROCA, Manuel, BURGUEÑO HURTADO, Javier, CIRUELA ALFÉREZ, Francisco. Development of a novel 1 receptor biosensor based on its heterodimerization with binding immunoglobulin protein in living cells. _ACS Chemical Neuroscience_. 2023. Vol. 14, núm. 2201-2207. [consulta: 25 de febrer de 2026]. ISSN: 1948-7193. [Disponible a: https://hdl.handle.net/2445/200655]