Agonist-independent and -dependent oligomerization of dopamine D(2) receptors by fusion to fluorescent proteins

FEBS Lett. 2001 Oct 19;507(1):109-13. doi: 10.1016/s0014-5793(01)02969-6.

Abstract

Oligomerization of the short (D(2S)) and long (D(2L)) isoforms of the dopamine D(2) receptor was explored in transfected Cos-7 cells by their C-terminal fusion to either an enhanced cyan or enhanced yellow fluorescent protein (ECFP or EYFP) and the fluorescent fusion protein interaction was monitored by a fluorescence resonance energy transfer (FRET) assay. The pharmacological properties of the fluorescent fusion proteins, as measured by both displacement of [(3)H]nemonapride binding and agonist-mediated stimulation of [(35)S]GTPgammaS binding upon co-expression with a G(alphao)Cys(351)Ile protein, were not different from the respective wild-type D(2S) and D(2L) receptors. Co-expression of D2S:ECFP+D2S:EYFP in a 1:1 ratio and D2L:ECFP+D2L:EYFP in a 27:1 ratio resulted, respectively, in an increase of 26% and 16% in the EYFP-specific fluorescent signal. These data are consistent with a close proximity of both D(2S) and D(2L) receptor pairs of fluorescent fusion proteins in the absence of ligand. The agonist-independent D(2S) receptor oligomerization could be attenuated by co-expression with either a wild-type, non-fluorescent D(2S) or D(2L) receptor subtype, but not with a distinct beta(2)-adrenoceptor. Incubation with the agonist (-)-norpropylapomorphine dose-dependently (EC(50): 0.23+/-0.06 nM) increased the FRET signal for the co-expression of D2S:ECFP and D2S:EYFP, in support of agonist-dependent D(2S) receptor oligomerization. In conclusion, our data strongly suggest the occurrence of dopamine D(2) receptor oligomers in intact Cos-7 cells.

MeSH terms

  • Animals
  • Apomorphine / analogs & derivatives*
  • Apomorphine / metabolism
  • Bacterial Proteins / chemistry
  • Bacterial Proteins / genetics
  • Bacterial Proteins / metabolism
  • Benzamides / metabolism
  • CHO Cells
  • COS Cells
  • Cricetinae
  • Dopamine Agonists / metabolism
  • Dopamine Antagonists / metabolism
  • Guanosine 5'-O-(3-Thiotriphosphate) / metabolism
  • Luminescent Proteins / chemistry
  • Luminescent Proteins / genetics
  • Luminescent Proteins / metabolism
  • Protein Structure, Quaternary
  • Receptors, Dopamine D2 / agonists*
  • Receptors, Dopamine D2 / chemistry*
  • Receptors, Dopamine D2 / genetics
  • Receptors, Dopamine D2 / metabolism
  • Recombinant Fusion Proteins / chemistry
  • Recombinant Fusion Proteins / genetics
  • Recombinant Fusion Proteins / metabolism
  • Transfection

Substances

  • Bacterial Proteins
  • Benzamides
  • Dopamine Agonists
  • Dopamine Antagonists
  • Luminescent Proteins
  • Receptors, Dopamine D2
  • Recombinant Fusion Proteins
  • yellow fluorescent protein, Bacteria
  • Guanosine 5'-O-(3-Thiotriphosphate)
  • N-n-propylnorapomorphine
  • Apomorphine
  • nemonapride