A unique role of the beta-2 thyroid hormone receptor isoform in negative regulation by thyroid hormone. Mapping of a novel amino-terminal domain important for ligand-independent activation

J Biol Chem. 1997 Oct 3;272(40):24927-33. doi: 10.1074/jbc.272.40.24927.

Abstract

Negative regulation by thyroid hormone is mediated by nuclear thyroid hormone receptors (TRs) acting on thyroid hormone response elements (TREs). We examine here the role of human TR-beta2, a TR isoform with central nervous system-restricted expression, in the regulation of target genes whose expression are decreased by triiodothyronine (T3). Using transient transfection studies, we found that TR-beta2 achieved significantly greater ligand-independent activation on the thyrotropin-releasing hormone (TRH) and common glycoprotein alpha-subunit genes than either TR-beta1 or TR-alpha1. A chimeric TR-beta isoform containing the TR-beta2 amino terminus linked to the TR-alpha1 DNA- and ligand-binding domains functioned like the TR-beta2 isoform on these promoters, confirming that the amino terminus of TR-beta2 was both necessary and sufficient to mediate this effect. By constructing deletion mutants of the TR-beta2 amino terminus, we demonstrate that amino acids 89-116 mediate this function. This domain, important in ligand-independent activation on negative TREs, is discrete from a previously described activation domain in the amino-terminal portion of TR-beta2. We conclude that the central nervous system-restricted TR-beta2 isoform has a unique effect on negative regulation by T3 that can be mapped to amino acids 89-116 of the amino terminus of the human TR-beta2.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Binding Sites
  • Cell Line
  • DNA-Binding Proteins
  • Fungal Proteins / biosynthesis
  • Gene Expression Regulation / drug effects
  • Humans
  • Luciferases / biosynthesis
  • Mice
  • Molecular Sequence Data
  • Promoter Regions, Genetic
  • Protein Biosynthesis
  • Rats
  • Receptors, Retinoic Acid / biosynthesis
  • Receptors, Thyroid Hormone / biosynthesis
  • Receptors, Thyroid Hormone / chemistry
  • Receptors, Thyroid Hormone / physiology*
  • Recombinant Fusion Proteins / biosynthesis
  • Recombinant Fusion Proteins / chemistry
  • Recombinant Fusion Proteins / metabolism
  • Retinoid X Receptors
  • Saccharomyces cerevisiae Proteins*
  • Sequence Alignment
  • Sequence Deletion
  • Sequence Homology, Amino Acid
  • Thyrotropin-Releasing Hormone / genetics
  • Transcription Factors / biosynthesis
  • Transcriptional Activation
  • Transfection
  • Triiodothyronine / pharmacology*

Substances

  • DNA-Binding Proteins
  • Fungal Proteins
  • GAL4 protein, S cerevisiae
  • Receptors, Retinoic Acid
  • Receptors, Thyroid Hormone
  • Recombinant Fusion Proteins
  • Retinoid X Receptors
  • Saccharomyces cerevisiae Proteins
  • Transcription Factors
  • Triiodothyronine
  • Thyrotropin-Releasing Hormone
  • Luciferases