Revealing a steroid receptor ligand as a unique PPARγ agonist.
In: Cell Research, Jg. 22 (2012-04-01), Heft 4, S. 746-756
academicJournal
Zugriff:
Peroxisome proliferator-activated receptor gamma (PPARγ) regulates metabolic homeostasis and is a molecular target for anti-diabetic drugs. We report here the identification of a steroid receptor ligand, RU-486, as an unexpected PPARγ agonist, thereby uncovering a novel signaling route for this steroid drug. Similar to rosiglitazone, RU-486 modulates the expression of key PPARγ target genes and promotes adipocyte differentiation, but with a lower adipogenic activity. Structural and functional studies of receptor-ligand interactions reveal the molecular basis for a unique binding mode for RU-486 in the PPARγ ligand-binding pocket with distinctive properties and epitopes, providing the molecular mechanisms for the discrimination of RU-486 from thiazolidinediones (TZDs) drugs. Our findings together indicate that steroid compounds may represent an alternative approach for designing non-TZD PPARγ ligands in the treatment of insulin resistance. [ABSTRACT FROM AUTHOR]
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Titel: |
Revealing a steroid receptor ligand as a unique PPARγ agonist.
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Autor/in / Beteiligte Person: | Lin, Shengchen ; Han, Ying ; Shi, Yuzhe ; Rong, Hui ; Zheng, Songyang ; Jin, Shikan ; Lin, Shu-Yong ; Lin, Sheng-Cai ; Li, Yong |
Zeitschrift: | Cell Research, Jg. 22 (2012-04-01), Heft 4, S. 746-756 |
Veröffentlichung: | 2012 |
Medientyp: | academicJournal |
ISSN: | 1001-0602 (print) |
DOI: | 10.1038/cr.2011.162 |
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