Literature DB >> 19914244

Structural activity relationship of flavonoids with estrogen-related receptor gamma.

Zhiyan Huang1, Fang Fang, Junjian Wang, Chi-Wai Wong.   

Abstract

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

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Year:  2010        PMID： 19914244     DOI： 10.1016/j.febslet.2009.11.026

Source DB:  PubMed          Journal:  FEBS Lett        ISSN： 0014-5793            Impact factor:   4.124


  13 in total

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