A G protein-coupled receptor and the intracellular synthase of its agonist functionally cooperate

J Cell Biol. 2014 Feb 3;204(3):377-93. doi: 10.1083/jcb.201304015.

Abstract

Export of newly synthesized G protein-coupled receptors (GPCRs) remains poorly characterized. We show in this paper that lipocalin-type prostaglandin D2 (PGD2) synthase (L-PGDS) interacts intracellularly with the GPCR DP1 in an agonist-independent manner. L-PGDS promotes cell surface expression of DP1, but not of other GPCRs, in HEK293 and HeLa cells, independent of L-PGDS enzyme activity. In addition, formation of a DP1-Hsp90 complex necessary for DP1 export to the cell surface is dependent on the interaction between L-PGDS and the C-terminal MEEVD residues of Hsp90. Surprisingly, PGD2 synthesis by L-PGDS is promoted by coexpression of DP1, suggesting a possible intracrine/autocrine signaling mechanism. In this regard, L-PGDS increases the formation of a DP1-ERK1/2 complex and increases DP1-mediated ERK1/2 signaling. Our findings define a novel cooperative mechanism in which a GPCR (DP1) promotes the activity of the enzyme (L-PGDS) that produces its agonist (PGD2) and in which this enzyme in turn acts as a cofactor (of Hsp90) to promote export and agonist-dependent activity of the receptor.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Membrane / metabolism
  • Cell Nucleus / enzymology
  • Enzyme Activation
  • Extracellular Signal-Regulated MAP Kinases / metabolism
  • HEK293 Cells
  • HSP90 Heat-Shock Proteins / metabolism
  • HeLa Cells
  • Humans
  • Intracellular Space / enzymology*
  • Intramolecular Oxidoreductases / metabolism*
  • Lipocalins / metabolism*
  • MAP Kinase Signaling System
  • Mutant Proteins / metabolism
  • Protein Transport
  • Receptors, G-Protein-Coupled / agonists*
  • Receptors, G-Protein-Coupled / metabolism*
  • Receptors, Prostaglandin / agonists*
  • Receptors, Prostaglandin / metabolism*
  • trans-Golgi Network / metabolism

Substances

  • HSP90 Heat-Shock Proteins
  • Lipocalins
  • Mutant Proteins
  • Receptors, G-Protein-Coupled
  • Receptors, Prostaglandin
  • prostanoid D receptor 1, human
  • Extracellular Signal-Regulated MAP Kinases
  • Intramolecular Oxidoreductases
  • prostaglandin R2 D-isomerase