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TR-binding activity of 3,5,3'-triiodo-L-thyronine (T3) was detectable at concentrations as low as 3.0 × 10-8 M and reached a plateau at 1.0 × 10-6 M. The concentration of T3 producing 10% of the activity stimulated at 1.0 × 10-6 M (10% relative effective concentration, REC10) was 2.1 × 10-8 M. 3,5,3',5'-tetraiodo-L-thyronine (T4), 3,3',5'-triiodo- L-thyronine (rT3) and 3, 5-diiodo-L-thyronine (T2) also exhibited TR-binding activities. The REC10 values of these chemicals were 4.2 × 10-8, 5.0 × 10-7 and 1.0 × 10-5 M, respectively. o-Isopropylphenol and o-t-butylphenol exhib- ited TR-binding activities with REC10 values of 3.1 × 10-4 and 4.8 × 10-5 M, respectively, whereas t-butylbenzene, isopropylbenzene and the other chemicals tested had no detectable TR-bindng activity. These results suggest that a phenolic hydroxyl group and the ortho-substituents may play important roles in the TR-binding activities of these chemicals. This assay system will be a useful tool for screening the TR-binding activities of chemicals.

Detection of Thyroid Hormone Receptor-Binding Activities of Chemicals Using a Yeast Two-Hybrid Assay.