FEBS Letters
Volume 584, Issue 1 , Pages 22-26, 4 January 2010

Structural activity relationship of flavonoids with estrogen-related receptor gamma

Edited by Robert Barouki

Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou Science City 510663, China

Received 28 September 2009; received in revised form 28 October 2009; accepted 7 November 2009. published online 13 November 2009.

Abstract 

In this study, we investigated the structural activity relationships (SARs) of flavonoids with estrogen-related receptor γ (ERRγ) and its coactivator peroxisome proliferators-activated receptor γ coactivator-1α (PGC-1α). Isoflavones (genistein and daidzein) and flavanones (naringenin and hesperetin) did not significantly affect ERRγ activity. Flavone apigenin and flavonol kaempferol directly suppressed the interaction between ERRγ and PGC-1α functioning as inverse agonists. In contrast, flavone luteolin suppressed PGC-1α activity in part through promoting the degradation of PGC-1α leading to suppressed ERRγ activity. Therefore, these flavones and flavonols utilize alternative mechanisms to influence the transcriptional activities of ERRγ and PGC-1α.

Structured summary

MINT-7297297, MINT-7297435: PGC-1 alpha NR2 (uniprotkb:Q9UBK2) binds (MI:0407) to ERR gamma (uniprotkb:P62508) by surface plasmon resonance (MI:0107)

Abbreviations: ERRγ, estrogen-related receptor γ, PGC-1α, peroxisome proliferators-activated receptor γ coactivator-1α, SAR, structural activity relationship

Keywords: Flavonoid, ERRγ, PGC-1α

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PII: S0014-5793(09)00928-4

doi:10.1016/j.febslet.2009.11.026

FEBS Letters
Volume 584, Issue 1 , Pages 22-26, 4 January 2010

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