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Study of the Sensing Kinetics of G Protein-Coupled Estrogen Receptor Sensors for Common Estrogens and Estrogen Analogs

Authors :
Dingqiang Lu
Xinqian Wang
Chunlei Feng
Danyang Liu
Yixuan Liu
Yujiao Liu
Jie Li
Jiayao Zhang
Na Li
Yujing Deng
Ke Wang
Ruijuan Ren
Guangchang Pang
Source :
Molecules, Vol 28, Iss 8, p 3286 (2023)
Publication Year :
2023
Publisher :
MDPI AG, 2023.

Abstract

Endogenous and exogenous estrogens are widely present in food and food packaging, and high levels of natural estrogens and the misuse or illegal use of synthetic estrogens can lead to endocrine disorders and even cancer in humans. Therefore, it is consequently important to accurately evaluate the presence of food-functional ingredients or toxins with estrogen-like effects. In this study, an electrochemical sensor based on G protein-coupled estrogen receptors (GPERs) was fabricated by self-assembly, modified by double-layered gold nanoparticles, and used to measure the sensing kinetics for five GPER ligands. The interconnected allosteric constants (Ka) of the sensor for 17β-estradiol, resveratrol, G-1, G-15, and bisphenol A were 8.90 × 10−17, 8.35 × 10−16, 8.00 × 10−15, 5.01 × 10−15, and 6.65 × 10−16 mol/L, respectively. The sensitivity of the sensor for the five ligands followed the order of 17β-estradiol > bisphenol A > resveratrol > G-15 > G-1. The receptor sensor also demonstrated higher sensor sensitivity for natural estrogens than exogenous estrogens. The results of molecular simulation docking showed that the residues Arg, Glu, His, and Asn of GPER mainly formed hydrogen bonds with -OH, C-O-C, or -NH-. In this study, simulating the intracellular receptor signaling cascade with an electrochemical signal amplification system enabled us to directly measure GPER–ligand interactions and explore the kinetics after the self-assembly of GPERs on a biosensor. This study also provides a novel platform for the accurate functional evaluation of food-functional components and toxins.

Details

Language :
English
ISSN :
14203049
Volume :
28
Issue :
8
Database :
Directory of Open Access Journals
Journal :
Molecules
Publication Type :
Academic Journal
Accession number :
edsdoj.1a6fbf9bed3f46aebad20034ba9dadef
Document Type :
article
Full Text :
https://doi.org/10.3390/molecules28083286