Identification of a binding motif specific to HNF4 by comparative analysis of multiple nuclear receptors

Nucleic Acids Res. 2012 Jul;40(12):5343-56. doi: 10.1093/nar/gks190. Epub 2012 Mar 1.

Abstract

Nuclear receptors (NRs) regulate gene expression by binding specific DNA sequences consisting of AG[G/T]TCA or AGAACA half site motifs in a variety of configurations. However, those motifs/configurations alone do not adequately explain the diversity of NR function in vivo. Here, a systematic examination of DNA binding specificity by protein-binding microarrays (PBMs) of three closely related human NRs--HNF4α, retinoid X receptor alpha (RXRα) and COUPTF2--reveals an HNF4-specific binding motif (H4-SBM), xxxxCAAAGTCCA, as well as a previously unrecognized polarity in the classical DR1 motif (AGGTCAxAGGTCA) for HNF4α, RXRα and COUPTF2 homodimers. ChIP-seq data indicate that the H4-SBM is uniquely bound by HNF4α but not 10 other NRs in vivo, while NRs PXR, FXRα, Rev-Erbα appear to bind adjacent to H4-SBMs. HNF4-specific DNA recognition and transactivation are mediated by residues Asp69 and Arg76 in the DNA-binding domain; this combination of amino acids is unique to HNF4 among all human NRs. Expression profiling and ChIP data predict ≈ 100 new human HNF4α target genes with an H4-SBM site, including several Co-enzyme A-related genes and genes with links to disease. These results provide important new insights into NR DNA binding.

Publication types

  • Comparative Study
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Arginine / chemistry
  • Aspartic Acid / chemistry
  • Binding Sites
  • COUP Transcription Factor II / metabolism
  • Hepatocyte Nuclear Factor 4 / chemistry
  • Hepatocyte Nuclear Factor 4 / metabolism*
  • Humans
  • Nucleotide Motifs
  • Protein Array Analysis
  • Protein Binding
  • Regulatory Elements, Transcriptional*
  • Retinoid X Receptor alpha / metabolism
  • Transcriptional Activation

Substances

  • COUP Transcription Factor II
  • HNF4A protein, human
  • Hepatocyte Nuclear Factor 4
  • Retinoid X Receptor alpha
  • Aspartic Acid
  • Arginine