A Cell-Based Method to Detect Agonist and Antagonist Activities of Endocrine-Disrupting Chemicals on GPER

一种基于细胞的方法来检测内分泌干扰化学物质对 GPER 的激动剂和拮抗剂活性

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作者:Séverine Périan, Catherine Cerutti, Christelle Forcet, Violaine Tribollet, Jean-Marc Vanacker

Abstract

Endocrine-disrupting chemicals (EDCs) are exogenous compounds that impact endogenous hormonal systems, resulting in adverse health effects. These chemicals can exert their actions by interfering with several pathways. Simple biological systems to determine whether EDCs act positively or negatively on a given receptor are often lacking. Here we describe a low-to-middle throughput method to screen the agonist/antagonist potential of EDCs specifically on the GPER membrane estrogen receptor. Application of this assay to 23 candidate EDCs from different chemical families reveals the existence of six agonists and six antagonists.

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