Environmental Monitoring and Contaminants Research
Online ISSN : 2435-7685
Articles
Evaluation of human thyroid receptor-agonist activity in 796 chemical compounds using a yeast two-hybrid assay with Saccharomyces cerevisiae Y190
Ryo OMAGARI Mayuko YAGISHITAMiho YAMASAKIRyo KAMATAMasanori TERASAKIFujio SHIRAISHITakuya KUBODaisuke NAKAJIMA
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2022 Volume 2 Pages 54-59

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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.

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