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http://hdl.handle.net/2445/200655
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DC Field | Value | Language |
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dc.contributor.author | Morató Arús, Xavier | - |
dc.contributor.author | Fernández Dueñas, Víctor | - |
dc.contributor.author | Pérez-Villamor, Pilar | - |
dc.contributor.author | Valle León, Marta | - |
dc.contributor.author | Vela, José Miguel | - |
dc.contributor.author | Merlos Roca, Manuel | - |
dc.contributor.author | Burgueño Hurtado, Javier | - |
dc.contributor.author | Ciruela Alférez, Francisco | - |
dc.date.accessioned | 2023-07-14T14:27:10Z | - |
dc.date.available | 2023-07-14T14:27:10Z | - |
dc.date.issued | 2023-12-01 | - |
dc.identifier.issn | 1948-7193 | - |
dc.identifier.uri | http://hdl.handle.net/2445/200655 | - |
dc.description.abstract | 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. | - |
dc.format.extent | 7 p. | - |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | American Chemical Society | - |
dc.relation.isformatof | Reproducció del document publicat a: https://doi.org/10.1021/acschemneuro.3c00206 | - |
dc.relation.ispartof | ACS Chemical Neuroscience, 2023, vol. 14, p. 2201-2207 | - |
dc.relation.uri | https://doi.org/10.1021/acschemneuro.3c00206 | - |
dc.rights | cc by (c) Morató Arús, Xavier, et al.; American Chemical Society, 2023 | - |
dc.rights.uri | https://creativecommons.org/licenses/by/4.0/ | - |
dc.source | Articles publicats en revistes (Patologia i Terapèutica Experimental) | - |
dc.subject.classification | Proteïnes portadores | - |
dc.subject.classification | Disseny de medicaments | - |
dc.subject.classification | Biosensors | - |
dc.subject.classification | Oligòmers | - |
dc.subject.other | Carrier proteins | - |
dc.subject.other | Drug design | - |
dc.subject.other | Biosensors | - |
dc.subject.other | Oligomers | - |
dc.title | Development of a novel 1 receptor biosensor based on its heterodimerization with binding immunoglobulin protein in living cells | - |
dc.type | info:eu-repo/semantics/article | - |
dc.type | info:eu-repo/semantics/publishedVersion | - |
dc.identifier.idgrec | 736463 | - |
dc.date.updated | 2023-07-14T14:27:10Z | - |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | - |
dc.identifier.pmid | 37191585 | - |
Appears in Collections: | Articles publicats en revistes (Patologia i Terapèutica Experimental) Articles publicats en revistes (Institut d'lnvestigació Biomèdica de Bellvitge (IDIBELL)) |
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736463.pdf | 2.14 MB | Adobe PDF | View/Open |
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