Competitive inhibition of T3 binding to alpha 1 and beta 1 thyroid hormone receptors by fatty acids

Biochem Biophys Res Commun. 1991 Sep 16;179(2):1011-6. doi: 10.1016/0006-291x(91)91919-4.

Abstract

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.

MeSH terms

  • Animals
  • Chickens
  • Electrophoresis, Polyacrylamide Gel
  • Escherichia coli / genetics
  • Fatty Acids / pharmacology*
  • Fatty Acids, Unsaturated / pharmacology
  • Hydrocarbons / chemistry
  • Kinetics
  • Plasmids
  • Proto-Oncogene Proteins / metabolism
  • Rats
  • Receptors, Thyroid Hormone / genetics
  • Receptors, Thyroid Hormone / metabolism*
  • Recombinant Fusion Proteins / metabolism
  • Triiodothyronine / antagonists & inhibitors
  • Triiodothyronine / metabolism*

Substances

  • Fatty Acids
  • Fatty Acids, Unsaturated
  • Hydrocarbons
  • Proto-Oncogene Proteins
  • Receptors, Thyroid Hormone
  • Recombinant Fusion Proteins
  • Triiodothyronine