Related Experiment Video
Updated: Jun 18, 2026

Screening for Phytoestrogens using a Cell-based Estrogen Receptor β Reporter Assay
Published on: June 7, 2020
Structural activity relationship of flavonoids with estrogen-related receptor gamma
Zhiyan Huang1, Fang Fang, Junjian Wang
1Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou Science City, China.
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.
More Related Videos
09:07Detecting the Ligand-binding Domain Dimerization Activity of Estrogen Receptor Alpha Using the Mammalian Two-Hybrid Assay
Published on: December 19, 2018
05:47In Silico Modeling Method for Computational Aquatic Toxicology of Endocrine Disruptors: A Software-Based Approach Using QSAR Toolbox
Published on: August 28, 2019
Related Concept Videos
Transducer Mechanism: Nuclear Receptors
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
The Two-State Receptor Model
The binding affinity of a drug determines its interaction with one...
Adrenergic Agonists: Chemistry and Structure-Activity Relationship
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of the aromatic...
Cholinergic Antagonists: Chemistry and Structure-Activity Relationship
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
Signal Transduction: Overview
Typically, signal transduction involves three...