Determinants of coactivator LXXLL motif specificity in nuclear receptor transcriptional activation

Genes Dev. 1998 Nov 1;12(21):3357-68. doi: 10.1101/gad.12.21.3357.

Abstract

Ligand-dependent activation of gene transcription by nuclear receptors is dependent on the recruitment of coactivators, including a family of related NCoA/SRC factors, via a region containing three helical domains sharing an LXXLL core consensus sequence, referred to as LXDs. In this manuscript, we report receptor-specific differential utilization of LXXLL-containing motifs of the NCoA-1/SRC-1 coactivator. Whereas a single LXD is sufficient for activation by the estrogen receptor, different combinations of two, appropriately spaced, LXDs are required for actions of the thyroid hormone, retinoic acid, peroxisome proliferator-activated, or progesterone receptors. The specificity of LXD usage in the cell appears to be dictated, at least in part, by specific amino acids carboxy-terminal to the core LXXLL motif that may make differential contacts with helices 1 and 3 (or 3') in receptor ligand-binding domains. Intriguingly, distinct carboxy-terminal amino acids are required for PPARgamma activation in response to different ligands. Related LXXLL-containing motifs in NCoA-1/SRC-1 are also required for a functional interaction with CBP, potentially interacting with a hydrophobic binding pocket. Together, these data suggest that the LXXLL-containing motifs have evolved to serve overlapping roles that are likely to permit both receptor-specific and ligand-specific assembly of a coactivator complex, and that these recognition motifs underlie the recruitment of coactivator complexes required for nuclear receptor function.

Publication types

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

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Cells, Cultured
  • Fibroblasts / cytology
  • Gene Expression Regulation
  • Histone Acetyltransferases
  • Models, Molecular
  • Molecular Sequence Data
  • Nuclear Proteins / physiology
  • Nuclear Receptor Coactivator 1
  • Peptide Fragments / chemistry*
  • Peptide Fragments / genetics
  • Peptide Fragments / physiology
  • Protein Structure, Secondary
  • Rats
  • Receptors, Cytoplasmic and Nuclear / chemistry*
  • Receptors, Cytoplasmic and Nuclear / genetics
  • Receptors, Steroid / chemistry
  • Receptors, Steroid / genetics
  • Sequence Alignment
  • Trans-Activators / physiology
  • Transcription Factors / chemistry*
  • Transcription Factors / genetics
  • Transcriptional Activation / physiology*

Substances

  • Nuclear Proteins
  • Peptide Fragments
  • Receptors, Cytoplasmic and Nuclear
  • Receptors, Steroid
  • Trans-Activators
  • Transcription Factors
  • Histone Acetyltransferases
  • Nuclear Receptor Coactivator 1