Publikationsserver der Universitätsbibliothek Marburg
Titel:Identifizierung und Charakterisierung des inversen PPARβ/δ-Agonisten DG172
Autor:Lieber, Sonja
Weitere Beteiligte: Müller, Rolf (Prof. Dr.)
Veröffentlicht:2014
URI:https://archiv.ub.uni-marburg.de/diss/z2014/0793
URN: urn:nbn:de:hebis:04-z2014-07932
DOI: https://doi.org/10.17192/z2014.0793
DDC: Biowissenschaften, Biologie
Titel (trans.):Identification and Characterization of the inverse PPARβ/δ Agonist DG172
Publikationsdatum:2015-01-05
Lizenz:https://rightsstatements.org/vocab/InC-NC/1.0/

Dokument

Schlagwörter:
Agonist, antagonist Hematopoiesis, Hämatopoese, agonist, nuclear receptor, Antagonist, Kernrezeptor

Zusammenfassung:
In den vergangenen Jahren konnten Nachweise erbracht werden, dass PPARβ/δ an einer Vielzahl schwerer Erkrankungen wie Krebs, Atherosklerose und Diabetes mellitus beteiligt ist. Eine mögliche therapeutische Option könnte daher eine Modulation dieses Rezeptors mittels spezifischer inhibitorischer Liganden sein. Zu Beginn der vorliegenden Arbeit waren zwar hochaffine PPARβ/δ-Agonisten verfügbar, jedoch waren alle beschriebenen inhibitorischen Liganden entweder nicht selektiv, nicht bioverfügbar oder zeigten eine pharmakologisch ungünstige, irreversible Interaktion mit PPARβ/δ. Zur Untersuchung des therapeutischen Potenzials von PPARβ/δ-Liganden war die Entwicklung neuer bioverfügbarer, selektiver inhibitorischer Liganden daher dringend geboten. Diese beinhalten sowohl Antagonisten, die durch eine Bindung an PPARβ/δ kompetitiv dessen Aktivität hemmen, als auch inverse Agonisten, die durch eine zusätzliche Rekrutierung von Corepressoren aktiv zu dessen Repressorfunktion beitragen.

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