LGR4 is a receptor for RANKL and negatively regulates osteoclast differentiation and bone resorption

Nat Med. 2016 May;22(5):539-46. doi: 10.1038/nm.4076. Epub 2016 Apr 11.

Abstract

Tumor necrosis factor (TNF) superfamily member 11 (TNFSF11, also known as RANKL) regulates multiple physiological or pathological functions, including osteoclast differentiation and osteoporosis. TNFRSF11A (also called RANK) is considered to be the sole receptor for RANKL. Herein we report that leucine-rich repeat-containing G-protein-coupled receptor 4 (LGR4, also called GPR48) is another receptor for RANKL. LGR4 competes with RANK to bind RANKL and suppresses canonical RANK signaling during osteoclast differentiation. RANKL binding to LGR4 activates the Gαq and GSK3-β signaling pathway, an action that suppresses the expression and activity of nuclear factor of activated T cells, cytoplasmic, calcineurin-dependent 1 (NFATC1) during osteoclastogenesis. Both whole-body (Lgr4(-/-)) and monocyte conditional knockout mice of Lgr4 (Lgr4 CKO) exhibit osteoclast hyperactivation (including elevation of osteoclast number, surface area, and size) and increased bone erosion. The soluble LGR4 extracellular domain (ECD) binds RANKL and inhibits osteoclast differentiation in vivo. Moreover, LGR4-ECD therapeutically abrogated RANKL-induced bone loss in three mouse models of osteoporosis. Therefore, LGR4 acts as a second RANKL receptor that negatively regulates osteoclast differentiation and bone resorption.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blotting, Western
  • Bone Remodeling / genetics*
  • Bone Resorption / genetics*
  • Calcium / metabolism
  • Cells, Cultured
  • Chromatin Immunoprecipitation
  • Enzyme-Linked Immunosorbent Assay
  • Flow Cytometry
  • GTP-Binding Protein alpha Subunits, Gq-G11 / metabolism
  • Giant Cell Tumor of Bone / metabolism
  • Glycogen Synthase Kinase 3 beta / metabolism
  • HEK293 Cells
  • Humans
  • Immunoprecipitation
  • Leukocytes, Mononuclear
  • Mice
  • Mice, Knockout
  • Molecular Docking Simulation
  • NFATC Transcription Factors / metabolism
  • Optical Imaging
  • Osteogenesis / genetics*
  • Osteoporosis / genetics
  • Osteoporosis / metabolism
  • RANK Ligand / metabolism*
  • RAW 264.7 Cells
  • Real-Time Polymerase Chain Reaction
  • Receptors, G-Protein-Coupled / genetics*
  • Signal Transduction
  • Surface Plasmon Resonance
  • X-Ray Microtomography

Substances

  • LGR4 protein, human
  • LGR4 protein, mouse
  • NFATC Transcription Factors
  • RANK Ligand
  • Receptors, G-Protein-Coupled
  • Glycogen Synthase Kinase 3 beta
  • GTP-Binding Protein alpha Subunits, Gq-G11
  • Calcium