Competitive inhibition of T3 binding to alpha 1 and beta 1 thyroid hormone receptors by fatty acids.
This study was undertaken to investigate whether fatty acids inhibit the binding of T3 to the alpha 1 and beta 1 form of the thyroid hormone receptor. Fatty acids inhibited the binding of T3 to both receptor proteins isolated from a bacterial expression system. The effectiveness of inhibition depends on the chain length and degree of saturation of the fatty acids. The inhibition of T3 binding to the alpha 1 and beta 1 receptor by oleic acid is competitive in nature; the Ki value was 5.4 10(-6) M for the c-erbA alpha 1 protein and 3.3 10(-6) M for the c-erb beta 1 protein. The findings indicate a direct interaction of fatty acids with T3 receptor proteins.
van der Klis
F R
FR
Division of Endocrinology, Academic Medical Centre, Amsterdam, The Netherlands.
Schmidt
E D
ED
van Beeren
H C
HC
Wiersinga
W M
WM
D000818:Animals; D002645:Chickens; D004591:Electrophoresis, Polyacrylamide Gel; D004926:Escherichia coli / Q000235:genetics; D005227:Fatty Acids / Q000494:pharmacology*; D005231:Fatty Acids, Unsaturated / Q000494:pharmacology; D006838:Hydrocarbons / Q000737:chemistry; D007700:Kinetics; D010957:Plasmids; D011518:Proto-Oncogene Proteins / Q000378:metabolism; D051381:Rats; D011988:Receptors, Thyroid Hormone / Q000235:genetics / Q000378:metabolism*; D011993:Recombinant Fusion Proteins / Q000378:metabolism; D014284:Triiodothyronine / Q000037:antagonists & inhibitors / Q000378:metabolism*
D005227:Fatty Acids; D005231:Fatty Acids, Unsaturated; D006838:Hydrocarbons; D011518:Proto-Oncogene Proteins; D011988:Receptors, Thyroid Hormone; D011993:Recombinant Fusion Proteins; D014284:Triiodothyronine