Targeting oxidative stress: novel coumarin-based inverse agonists of GPR55
Abstract: Oxidative stress is associated with different neurological and psychiatric diseases. Therefore, development of new pharmaceuticals targeting oxidative dysregulation might be a promising approach to treat these diseases. The G-protein coupled receptor 55 (GPR55) is broadly expressed in central nervous tissues and cells and is involved in the regulation of inflammatory and oxidative cell homeostasis. We have recently shown that coumarin-based compounds enfold inverse agonistic activities at GPR55 resulting in the inhibition of prostaglandin E2. However, the antioxidative effects mediated by GPR55 were not evaluated yet. Therefore, we investigated the antioxidative effects of two novel synthesized coumarin-based compounds, KIT C and KIT H, in primary mouse microglial and human neuronal SK-N-SK cells. KIT C and KIT H show antioxidative properties in SK-N-SH cells as well as in primary microglia. In GPR55-knockout SK-N-SH cells, the antioxidative effects are abolished, suggesting a GPR55-dependent antioxidative mechanism. Since inverse agonistic GPR55 activation in the brain seems to be associated with decreased oxidative stress, KIT C and KIT H possibly act as inverse agonists of GPR55 eliciting promising therapeutic options for oxidative stress related diseases
- Location
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Deutsche Nationalbibliothek Frankfurt am Main
- Extent
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Online-Ressource
- Language
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Englisch
- Notes
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International journal of molecular sciences. - 22, 21 (2021) , 11665, ISSN: 1422-0067
- Event
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Veröffentlichung
- (where)
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Freiburg
- (who)
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Universität
- (when)
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2021
- Creator
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Apweiler, Matthias
Saliba, Soraya Wilke
Streyczek, Jana
Hurrle, Thomas
Gräßle, Simone
Bräse, Stefan
Fiebich, Bernd L.
- DOI
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10.3390/ijms222111665
- URN
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urn:nbn:de:bsz:25-freidok-2225731
- Rights
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Kein Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
- Last update
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25.03.2025, 1:48 PM CET
Data provider
Deutsche Nationalbibliothek. If you have any questions about the object, please contact the data provider.
Associated
- Apweiler, Matthias
- Saliba, Soraya Wilke
- Streyczek, Jana
- Hurrle, Thomas
- Gräßle, Simone
- Bräse, Stefan
- Fiebich, Bernd L.
- Universität
Time of origin
- 2021
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