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https://hdl.handle.net/2445/217146
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DC Field | Value | Language |
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dc.contributor.author | Peyman, Mona | - |
dc.contributor.author | Barroso Fernández, Emma | - |
dc.contributor.author | Turcu, Andreea L. | - |
dc.contributor.author | Estrany Jr, Francesc | - |
dc.contributor.author | Smith, Dáire | - |
dc.contributor.author | Jurado Aguilar, Javier | - |
dc.contributor.author | Rada, Patricia | - |
dc.contributor.author | Morisseau, Christophe | - |
dc.contributor.author | Hammock, Bruce D. | - |
dc.contributor.author | Valverde, Ángela M. | - |
dc.contributor.author | Palomer Tarridas, Francesc Xavier | - |
dc.contributor.author | Galdeano Cantador, Carlos | - |
dc.contributor.author | Vázquez Cruz, Santiago | - |
dc.contributor.author | Vázquez Carrera, Manuel | - |
dc.date.accessioned | 2024-12-17T11:58:41Z | - |
dc.date.available | 2024-12-17T11:58:41Z | - |
dc.date.issued | 2023-10-11 | - |
dc.identifier.issn | 0753-3322 | - |
dc.identifier.uri | https://hdl.handle.net/2445/217146 | - |
dc.description.abstract | Soluble epoxide hydrolase (sEH) is a drug target with the potential for therapeutic utility in the areas of inflammation, neurodegenerative disease, chronic pain, and diabetes, among others. Proteolysis-targeting chimeras (PROTACs) molecules offer new opportunities for targeting sEH, due to its capacity to induce its degradation. Here, we describe that the new ALT-PG2, a PROTAC that degrades sEH protein in the human hepatic Huh-7 cell line, in isolated mouse primary hepatocytes, and in the liver of mice. Remarkably, sEH degradation caused by ALT-PG2 was accompanied by an increase in the phosphorylated levels of AMP-activated protein kinase (AMPK), while phosphorylated extracellular-signal-regulated kinase 1/2 (ERK1/2) was reduced. Consistent with the key role of these kinases on endoplasmic reticulum (ER) stress, ALT-PG2 attenuated the levels of ER stress and inflammatory markers. Overall, the findings of this study indicate that targeting sEH with degraders is a promising pharmacological strategy to promote AMPK activation and to reduce ER stress and inflammation. | - |
dc.format.extent | 1 p. | - |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | Elsevier Masson SAS | - |
dc.relation.isformatof | Reproducció del document publicat a: https://doi.org/10.1016/j.biopha.2023.115667 | - |
dc.relation.ispartof | Biomedicine & Pharmacotherapy, 2023, vol. 168, p. 115667 | - |
dc.relation.uri | https://doi.org/10.1016/j.biopha.2023.115667 | - |
dc.rights | cc by-nc-nd (c) Mona Peyman, et al., 2023 | - |
dc.rights.uri | http://creativecommons.org/licenses/by-nc-nd/3.0/es/ | * |
dc.source | Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica) | - |
dc.subject.classification | Epòxids | - |
dc.subject.classification | Inflamació | - |
dc.subject.classification | Neurologia | - |
dc.subject.other | Epoxy compounds | - |
dc.subject.other | Inflammation | - |
dc.subject.other | Neurology | - |
dc.title | Soluble epoxide hydrolase-targeting PROTAC activates AMPK and inhibits endoplasmic reticulum stress | - |
dc.type | info:eu-repo/semantics/article | - |
dc.type | info:eu-repo/semantics/publishedVersion | - |
dc.identifier.idgrec | 739794 | - |
dc.date.updated | 2024-12-17T11:58:41Z | - |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | - |
Appears in Collections: | Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica) Articles publicats en revistes (Institut de Biomedicina (IBUB)) |
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833218.pdf | 4.38 MB | Adobe PDF | View/Open |
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