研究業績

Environmental Monitoring and Contaminants Research 2, 54-59 (2022)
Evaluation of human thyroid receptor-agonist activity in 796 chemical compounds using a yeast two-hybrid assay with Saccharomyces cerevisiae Y190

著者

Ryo OMAGARI, Mayuko YAGISHITA, Miho YAMASAKI, Ryo KAMATA, Masanori TERASAKI, Fujio SHIRAISHI, Takuya KUBO, and Daisuke NAKAJIMA

カテゴリ

学術論文

Abstract

The human thyroid receptor (hTR)-agonist activities of 796 compounds were evaluated using a yeast two-hybrid assay in this study. A total of 17 compounds exhibited agonist activity at tenfold the effective concentration (EC×10) [0.0083–7,500 nM]. Additionally, TRIAC, TETRAC, and GC-1, which exhibited 30–200 times higher activities than T3 and T4, may cause thyroid-hormone receptors (TR) activity at extremely low concentrations in real environmental water. Moreover, 3-chloro-3’,5,5’-triiodo-L-thyronine exhibited high TR-agonist activity for the first time. Chemicals with a structure equivalent to thyroid hormones exhibited TR-agonist activity regardless of the TR type. Information on hTR-agonist activity is important because previous studies, such as those involving EDSP21, have focused exclusively on rTR-agonist activity. Therefore, the knowledge gained from the present study will boost chemical regulation strategies benefiting human and wildlife.