Role of an AP-2-like element in transcriptional regulation of mouse mu-opioid receptor gene

Brain Res Mol Brain Res. 2003 Apr 10;112(1-2):153-62. doi: 10.1016/s0169-328x(03)00086-x.

Abstract

Previously, several important cis-elements and trans-factors have been shown to play a functional role in the proximal promoter of mouse mu-opioid receptor (MOR) gene. In this study, we defined another functional element located the in -450 to -400 bp (translational start site designated as +1) region of the proximal promoter, which is also essential for the full promoter activity. It is designated as the morAP-2-like element for its sequence homologous to the consensus AP-2 element. Surprisingly, electrophoretic mobility shift analysis (EMSA) revealed that Sp1 and Sp3, but not AP-2 proteins, were specifically bound to the morAP-2-like element. Mutation of the morAP-2-like element, resulting in a loss of Sp binding, led to an approximately 35% decrease in activity, further confirming the positive role of the morAP-2-like element in MOR gene expression. Dephosphorylation of Sp proteins with alkaline phosphatase also decreased Sp binding to the morAP-2-like element in EMSA, suggesting phosphorylation of Sp is essential for its binding to this element. However, direct or indirect activation of PKA, a classical G-protein coupled signaling pathway, resulted in no significant change of Sp binding to the morAP-2-like element, nor of the promoter activity the SH-SY5Y cells, MOR expressing cells, suggesting that phosphorylation of Sp does not involve PKA. These results suggest that the binding of different phosphorylated forms of Sp proteins to the morAP-2-like element may contribute to the fine tuning of MOR expression in different cells.

Publication types

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

MeSH terms

  • Animals
  • Base Sequence / genetics
  • Central Nervous System / metabolism*
  • Cyclic AMP-Dependent Protein Kinases / drug effects
  • Cyclic AMP-Dependent Protein Kinases / metabolism
  • DNA-Binding Proteins / genetics*
  • Down-Regulation / genetics
  • Gene Expression Regulation / genetics
  • Genes, Regulator / genetics*
  • Humans
  • Kruppel-Like Transcription Factors
  • Mice
  • Molecular Sequence Data
  • Neurons / metabolism*
  • Opioid Peptides / metabolism*
  • Phosphorylation
  • Promoter Regions, Genetic / genetics
  • Protein Binding / genetics
  • Protein Biosynthesis / genetics
  • Receptors, Opioid, mu / biosynthesis*
  • Receptors, Opioid, mu / genetics
  • Sp1 Transcription Factor / genetics
  • Sp1 Transcription Factor / metabolism
  • Transcription Factors / genetics*
  • Tumor Cells, Cultured

Substances

  • DNA-Binding Proteins
  • KLF12 protein, human
  • Kruppel-Like Transcription Factors
  • Opioid Peptides
  • Receptors, Opioid, mu
  • Sp1 Transcription Factor
  • Transcription Factors
  • Cyclic AMP-Dependent Protein Kinases