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dc.contributor.authorÅstrand, Ove Alexander Høgmoen
dc.contributor.authorViktorsson, Elvar Örn
dc.contributor.authorKristensen, Aleksander Lim
dc.contributor.authorEkeberg, Dag
dc.contributor.authorRøberg-Larsen, Hanne
dc.contributor.authorWilson, Steven Ray Haakon
dc.contributor.authorGabrielsen, Mari
dc.contributor.authorSylte, Ingebrigt
dc.contributor.authorRustan, Arild
dc.contributor.authorThoresen, G. Hege
dc.contributor.authorRongved, Pål
dc.contributor.authorKase, Eili Tranheim
dc.date.accessioned2018-11-01T10:49:03Z
dc.date.available2018-11-01T10:49:03Z
dc.date.issued2016-07-26
dc.description.abstractLiver X Receptor (LXR) modulators have shown potential as drugs since they target genes affecting metabolism and fatty acid synthesis. LXR antagonists are of particular interest since they are able to reduce the synthesis of complex fatty acids and glucose uptake. Based on molecular modeling, five new cholesterol mimics were synthesized, where four contained a hydroxyl group in the 22-S-position. The new compounds were screened in vitro against several genes affecting lipid metabolism. The compound that performed best in vitro was a dimethylamide derivative of 22(S)-hydroxycholesterol and it was chosen for in vivo testing. However, the blood plasma analysis from the in vivo tests revealed a concentration lower than needed to give any response, indicating either rapid metabolism or low bioavailability.en_US
dc.description.sponsorshipUniversity of Oslo Notur/NorStoreen_US
dc.descriptionAccepted manuscript version. Published version available at <a href=https://doi.org/10.1016/j.jsbmb.2016.07.010> https://doi.org/10.1016/j.jsbmb.2016.07.010</a>. Licensed <a href=http://creativecommons.org/licenses/by-nc-nd/4.0/> CC BY-NC-ND 4.0.</a>en_US
dc.identifier.citationÅstrand, O.A.H., Viktorsson, E.Ö., Kristensen, A.L., Ekeberg, D., Røberg-Larsen, H. Wilson, S.R., ... Kase, E.T. (2017). Synthesis, in vitro and in vivo biological evaluation of new oxysterols as modulators of the liver X receptors. Journal of Steroid Biochemistry and Molecular Biology, 165, 323-330. https://doi.org/10.1016/j.jsbmb.2016.07.010en_US
dc.identifier.cristinIDFRIDAID 1379848
dc.identifier.doi10.1016/j.jsbmb.2016.07.010
dc.identifier.issn0960-0760
dc.identifier.issn1879-1220
dc.identifier.urihttps://hdl.handle.net/10037/14073
dc.language.isoengen_US
dc.publisherElsevieren_US
dc.relation.journalJournal of Steroid Biochemistry and Molecular Biology
dc.rights.accessRightsopenAccessen_US
dc.subjectVDP::Medical disciplines: 700::Basic medical, dental and veterinary science disciplines: 710::Medical molecular biology: 711en_US
dc.subjectVDP::Medisinske Fag: 700::Basale medisinske, odontologiske og veterinærmedisinske fag: 710::Medisinsk molekylærbiologi: 711en_US
dc.subjectSteroid synthesisen_US
dc.subjectNuclear receptor modulationen_US
dc.subjectMolecular modellingen_US
dc.subjectBiological evaluationen_US
dc.titleSynthesis, in vitro and in vivo biological evaluation of new oxysterols as modulators of the liver X receptorsen_US
dc.typeJournal articleen_US
dc.typeTidsskriftartikkelen_US
dc.typePeer revieweden_US


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