Evaluation of human thyroid hormone receptor-antagonist activity in 691 chemical compounds using a yeast two-hybrid assay with Saccharomyces cerevisiae Y190

The human thyroid receptor (hTR)-antagonist activities of 691 compounds were evaluated using a yeast two-hybrid assay with Saccharomyces cerevisiae Y190 introduced hTR alpha and coactivator. In parallel, those YTOX tests were conducted to evaluate whether those compounds affected either antagonism or toxicity. This is the first report that focuses on the hTR-antagonist activity of many chemical compounds suspected to be endocrine disruptor. In this study, 46 compounds exhibited antagonist activity at 50% of the maximum activity (IC x 50) within 11-9940 nM. In particular, 10,10-Oxybisphenoxarsine, triphenyltin fluoride, triphenyltin hydroxide, and chlorothalonil had strong hTR-antagonist activities. This knowledge gained from the present study will boost chemical regulation strategies for human and wildlife health. (C) 2022 The Author(s). Published by Elsevier Inc.

Automated summary

This study is the first report on the hTR-antagonist activity of many chemical compounds suspected to be endocrine disruptors. The research found that 46 compounds exhibited antagonist activity, with 10,10-Oxybisphenoxarsine, triphenyltin fluoride, triphenyltin hydroxide, and chlorothalonil showing strong hTR-antagonist activities. The knowledge gained from this study will have significant implications for chemical regulation strategies for human and wildlife health.