GPR177 in A-fiber sensory neurons drives diabetic neuropathic pain via WNT-mediated TRPV1 activation

Sci Transl Med. 2022 Apr 6;14(639):eabh2557. doi: 10.1126/scitranslmed.abh2557. Epub 2022 Apr 6.

Abstract

Diabetic neuropathic pain (DNP) is a common and devastating complication in patients with diabetes. The mechanisms mediating DNP are not completely elucidated, and effective treatments are lacking. A-fiber sensory neurons have been shown to mediate the development of mechanical allodynia in neuropathic pain, yet the molecular basis underlying the contribution of A-fiber neurons is still unclear. Here, we report that the orphan G protein-coupled receptor 177 (GPR177) in A-fiber neurons drives DNP via WNT5a-mediated activation of transient receptor potential vanilloid receptor-1 (TRPV1) ion channel. GPR177 is mainly expressed in large-diameter A-fiber dorsal root ganglion (DRG) neurons and required for the development of DNP in mice. Mechanistically, we found that GPR177 mediated the secretion of WNT5a from A-fiber DRG neurons into cerebrospinal fluid (CSF), which was necessary for the maintenance of DNP. Extracellular perfusion of WNT5a induced rapid currents in both TRPV1-expressing heterologous cells and nociceptive DRG neurons. Computer simulations revealed that WNT5a has the potential to bind the residues at the extracellular S5-S6 loop of TRPV1. Using a peptide able to disrupt the predicted WNT5a/TRPV1 interaction suppressed DNP- and WNT5a-induced neuropathic pain symptoms in rodents. We confirmed GPR177/WNT5A coexpression in human DRG neurons and WNT5A secretion in CSF from patients with DNP. Thus, our results reveal a role for WNT5a as an endogenous and potent TRPV1 agonist, and the GPR177-WNT5a-TRPV1 axis as a driver of DNP pathogenesis in rodents. Our findings identified a potential analgesic target that might relieve neuropathic pain in patients with diabetes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Diabetes Mellitus* / metabolism
  • Diabetic Neuropathies* / metabolism
  • Ganglia, Spinal / metabolism
  • Humans
  • Intracellular Signaling Peptides and Proteins* / metabolism
  • Mice
  • Neuralgia* / metabolism
  • Receptors, G-Protein-Coupled* / metabolism
  • Sensory Receptor Cells / metabolism
  • TRPV Cation Channels* / metabolism
  • Wnt-5a Protein* / metabolism

Substances

  • Gpr177 protein, mouse
  • Intracellular Signaling Peptides and Proteins
  • Receptors, G-Protein-Coupled
  • TRPV Cation Channels
  • TRPV1 protein, human
  • TRPV1 protein, mouse
  • WLS protein, human
  • Wnt-5a Protein