The orphan GPCR GPR87 was deorphanized and shown to be a lysophosphatidic acid receptor

Biochem Biophys Res Commun. 2007 Nov 23;363(3):861-6. doi: 10.1016/j.bbrc.2007.09.063. Epub 2007 Sep 24.


In CHO cells stably expressing the GPR87 fused with a G16alpha protein, lysophosphatidic acid (LPA) evoked an intracellular Ca(2+) increase in a high affinity manner. The Ca(2+) increase was reversibly blocked by the LPA receptor antagonists and inhibited by pretreatment of the cells with GPR87-specific siRNAs. GPR87 was shown to be closer to the P2Y and P2Y-related receptors than LPA receptors by ClustalW analyses. However, none of nucleotides and their derivatives activated GPR87. The human gpr87 is located on the chromosome 3q25 in a cluster containing p2y12,13,14. RT-PCR analysis showed that the mouse GPR87 was expressed in placenta, ovary, testis, prostate, brain, and skeletal muscle. The 3D model of GPR87-LPA complex indicated that the ligand interacted with R115 and K296 of GPR87, which are well conserved in the P2Y receptors. These results suggest that the GPR87 is a LPA receptor which evolved from a common ancestor of P2Y receptors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Binding Sites / genetics
  • CHO Cells
  • Calcium / metabolism*
  • Cricetinae
  • Cricetulus
  • Electrophoresis, Polyacrylamide Gel
  • Female
  • GTP-Binding Protein alpha Subunits / genetics
  • GTP-Binding Protein alpha Subunits / metabolism
  • Gene Expression Profiling
  • Humans
  • Intracellular Fluid / drug effects
  • Intracellular Fluid / metabolism
  • Isoxazoles / pharmacology
  • Lysophospholipids / metabolism
  • Lysophospholipids / pharmacology
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Models, Molecular
  • Propionates / pharmacology
  • Protein Structure, Tertiary
  • RNA Interference
  • Receptors, G-Protein-Coupled / chemistry
  • Receptors, G-Protein-Coupled / genetics
  • Receptors, G-Protein-Coupled / metabolism*
  • Receptors, Lysophosphatidic Acid / antagonists & inhibitors
  • Receptors, Lysophosphatidic Acid / genetics
  • Receptors, Lysophosphatidic Acid / metabolism*
  • Recombinant Fusion Proteins / genetics
  • Recombinant Fusion Proteins / metabolism
  • Reverse Transcriptase Polymerase Chain Reaction
  • Uridine Triphosphate / pharmacology


  • 3-(4-(4-((1-(2-chlorophenyl)ethoxy)carbonyl amino)-3-methyl-5-isoxazolyl) benzylsulfanyl) propanoic acid
  • GPR87 protein, human
  • GPR87 protein, mouse
  • GTP-Binding Protein alpha Subunits
  • Isoxazoles
  • Lysophospholipids
  • Propionates
  • Receptors, G-Protein-Coupled
  • Receptors, Lysophosphatidic Acid
  • Recombinant Fusion Proteins
  • lysophosphatidic acid
  • Calcium
  • Uridine Triphosphate