Kaempferol is an estrogen-related receptor α and γ inverse agonist

Abstract 

Kaempferol is a dietary flavonoid that is thought to function as a selective estrogen receptor modulator. In this study, we established that kaempferol also functions as an inverse agonist for estrogen-related receptors alpha and gamma (ERRα and ERRγ). We demonstrated that kaempferol binds to ERRα and ERRγ and blocks their interaction with coactivator peroxisome proliferator-activated receptor γ coactivator-1α (PGC-1α). Kaempferol also suppressed the expressions of ERR-target genes pyruvate dehydrogenase kinase 2 and 4 (PDK2 and PDK4). This evidence suggests that kaempferol may exert some of its biological effect through both estrogen receptors and estrogen-related receptors.

Structured summary:

MINT-6824653:

PGC-1 alpha (uniprotkb:Q9UBK2) and ERR gamma (uniprotkb: P62508) bind (MI:0407) by surface plasmon resonance (MI:0107)

Abbreviations: ERR, estrogen-related receptor, ER, estrogen receptor, PGC-1α, peroxisome proliferator-activated receptor γ coactivator-1α, LBD, ligand binding domains, 4-OHT, 4-hydroxytamoxifene, RU, resonance units, SPR, surface plasmon resonance, PDK, pyruvate dehydrogenase kinase

Keywords: Estrogen receptor, Estrogen-related receptor, Kaempferol