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736463.pdf (2.09 MB)

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2023-12-01

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cc by (c) Morató Arús, Xavier, et al.; American Chemical Society, 2023
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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Recurs relacionat

https://doi.org/10.1021/acschemneuro.3c00206

Resum

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.

Matèries

Proteïnes portadores, Disseny de medicaments, Biosensors, Oligòmers

Matèries (anglès)

Carrier proteins, Drug design, Biosensors, Oligomers

Citació

Col·leccions

Articles publicats en revistes (Patologia i Terapèutica Experimental)
Articles publicats en revistes (Institut d'lnvestigació Biomèdica de Bellvitge (IDIBELL))

Citació

MORATÓ ARÚS, Xavier, et al. Development of a novel 1 receptor biosensor based on its heterodimerization with binding immunoglobulin protein in living cells. ACS Chemical Neuroscience. 2023. Vol. 14, num. 2201-2207. ISSN 1948-7193. [consulted: 17 of August of 2026]. Available at: https://hdl.handle.net/2445/200655

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