Thyroid hormone receptor/and v-erbA. A single amino acid difference in the C-terminal region influences dominant negative activity and receptor dimer formation

J Biol Chem. 1991 Jun 25;266(18):11589-93.

Abstract

Thyroid hormone receptors are cellular homologues (c-erbAs) of the v-erbA oncoprotein of the avian erythroblastosis virus. Exclusive of the viral gag region, v-erbA differs from the chick c-erbA-alpha receptor by two amino acid changes N-terminal of the DNA binding domain, two amino acid changes in the DNA binding domain, nine amino acid changes in the C-terminal region corresponding to the ligand binding domain of c-erbA, and a nine-amino acid deletion near the C terminus. v-erbA does not bind thyroid hormone and when expressed in cells inhibits the activity of wild-type thyroid hormone receptors. We reported previously that mutants of chick c-erbA/thyroid hormone receptor which lack the DNA binding domain (DBD-) inhibit transcriptional activition by wild-type thyroid hormone and retinoic acid receptors (Forman, B. M., Yang, C.-R., Au, M., Casanova, J., Ghysdael, J., and Samuels, H. H. (1989) Mol. Endocrinol. 3, 1610-1626). This dominant negative activity mapped to a series of hydrophobic heptad motifs which are conserved in the C terminus of these receptors and have been suggested to play a role in receptor dimerization. In this study we show that unlike DBD- c-erbA, DBD- v-erbA does not block receptor activity, suggesting that v-erbA acts by competing for DNA response elements rather than by formation of nonfunctional v-erbA/c-erbA heterodimers. This difference in activity was localized to a single Pro to Ser change in v-erbA just N-terminal of the last heptad motif. Introduction of this Pro to Ser change into DBD- c-erbA resulted in a protein which was inactive both functionally and in blocking receptor dimer formation in vitro.

Publication types

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

MeSH terms

  • Alpharetrovirus / genetics*
  • Amino Acids / genetics
  • Animals
  • Carrier Proteins / metabolism
  • Chickens
  • Chimera
  • DNA, Viral / metabolism
  • Gene Expression Regulation, Viral
  • Genes, Viral
  • HeLa Cells
  • Humans
  • Mutation
  • Oncogene Proteins v-erbA
  • Plasmids
  • Precipitin Tests
  • Proto-Oncogene Proteins / genetics*
  • Receptors, Retinoic Acid
  • Receptors, Thyroid Hormone / genetics*
  • Receptors, Thyroid Hormone / metabolism
  • Retroviridae Proteins, Oncogenic / genetics*
  • Transcriptional Activation

Substances

  • Amino Acids
  • Carrier Proteins
  • DNA, Viral
  • Oncogene Proteins v-erbA
  • Proto-Oncogene Proteins
  • Receptors, Retinoic Acid
  • Receptors, Thyroid Hormone
  • Retroviridae Proteins, Oncogenic