Identification of cis-elements of the human endothelin-A receptor gene and inhibition of the gene expression by the decoy strategy

J Biol Chem. 1998 Jun 26;273(26):15993-9. doi: 10.1074/jbc.273.26.15993.

Abstract

Previously, we succeeded in molecular cloning of the cDNA and the gene for human endothelin-A receptor (ET-AR). In the present study, we define cis-elements in the 5'-flanking region of the ET-AR gene. Deletion analyses were performed in A7r5 cells, rat vascular smooth muscle cell line, and Chinese hamster ovary cells using ET-AR promoter-luciferase gene constructs including 5 kilobases of the 5'-flanking region. These analyses demonstrated the existence of one negative regulatory element (-2.0 kilobases to -857 bases) and two positive regulatory elements (-137 to -53 and -53 to +251). Gel mobility shift assay revealed a nuclear protein binding to the region (-104 to -78) (R1). DNase I footprinting analysis showed a footprint spanning from -91 to -83 whose sequence is CCCCACCTT (ETA-P1). When a plasmid including R1 fragments (R1 decoy) was co-transfected into A7r5 cells with ET-AR (-137 to +251)-luciferase gene construct, it significantly reduced the luciferase activity in a dose-dependent manner. Moreover, R1 decoy down-regulated the endogenous ET-AR mRNA in A7r5 cells by a maximum of 75%. Thus, we identified cis-elements that regulate basal transcriptional activity of the ET-AR gene and proved the feasibility to suppress the expression of the ET-AR gene by the DNA decoy strategy using the positive regulatory element we identified.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apolipoproteins E / genetics
  • Base Sequence
  • Binding Sites
  • CHO Cells
  • Cricetinae
  • DNA Footprinting
  • Enhancer Elements, Genetic*
  • Gene Expression Regulation*
  • Humans
  • Molecular Sequence Data
  • Peptides, Cyclic / metabolism
  • Promoter Regions, Genetic
  • Rats
  • Receptor, Endothelin A
  • Receptors, Endothelin / genetics*
  • Transcription, Genetic
  • Transfection

Substances

  • Apolipoproteins E
  • Peptides, Cyclic
  • Receptor, Endothelin A
  • Receptors, Endothelin
  • cyclo(Trp-Asp-Pro-Val-Leu)

Associated data

  • GENBANK/AB012724