Molecular basis for gene-specific transactivation by nuclear receptors

Biochim Biophys Acta. 2011 Aug;1812(8):824-35. doi: 10.1016/j.bbadis.2010.12.018. Epub 2010 Dec 28.

Abstract

Nuclear receptors (NRs) are key transcriptional regulators of metazoan physiology and metabolism. Different NRs bind to similar or even identical core response elements; however, they regulate transcription in a highly receptor- and gene-specific manner. These differences in gene activation can most likely be accounted for by mechanisms involving receptor-specific interactions with DNA as well as receptor-specific interactions with protein complexes binding to adjacent and distant DNA sequences. Here, we review key molecular aspects of transactivation by NRs with special emphasis on the recent advances in the molecular mechanisms responsible for receptor- and gene-specific transcriptional activation. This article is part of a Special Issue entitled: Translating nuclear receptors from health to disease.

Publication types

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

MeSH terms

  • Amino Acid Sequence
  • Binding Sites
  • Humans
  • Ligands
  • Models, Molecular
  • Molecular Sequence Data
  • Protein Conformation
  • Receptor Cross-Talk
  • Receptors, Cytoplasmic and Nuclear / chemistry
  • Receptors, Cytoplasmic and Nuclear / metabolism
  • Receptors, Cytoplasmic and Nuclear / physiology*
  • Transcriptional Activation / genetics*

Substances

  • Ligands
  • Receptors, Cytoplasmic and Nuclear