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Identifizierung und Charakterisierung des inversen PPARβ/δ-Agonisten DG172
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 Lig...
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| Format: | Dissertation |
| Sprache: | Deutsch |
| Veröffentlicht: |
Philipps-Universität Marburg
2014
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| Schlagworte: | |
| Online Zugang: | PDF-Volltext |
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Research of the past years has provided clear evidence that PPARβ/δ is associated with major diseases including cancer, atherosclerosis and diabetes mellitus. Modulation of this receptor by specific inhibitory ligands represents a potential therapeutic option. At the beginning of this work highly affine agonists for PPARβ/δ were available, but all described inhibitory ligands were either not selective, not bioavailable or showed a pharmacologically undesirable, irreversible interaction with PPARβ/δ. To investigate the therapeutic potential of PPARβ/δ ligands the development of new was highly desirable. These include antagonists, which inhibit PPARβ/δ activity by competition with endogenous ligands, and inverse agonists, which actively trigger corepressor recruitment and establishment of an active transcriptional repressor complex.