Neurokinin-1 receptor is a novel positive regulator of Wnt/ β-catenin signaling in melanogenesis

Oncotarget. 2016 Dec 6;7(49):81268-81280. doi: 10.18632/oncotarget.13222.

Abstract

Wnt/β-catenin signaling is essential for melanogenesis in melanocytes. Neurokinin-1 receptor (NK-1R) has recently been demonstrated to be involved in melanin production. However, the cross talk between NK-1R and Wnt/β-catenin is poorly understood. Here, [Sar9, Met(O2)11] substance P (SMSP) was used to activate NK-1R, while L-733060 was used to inhibit it. The effects of NK-1R activation and inhibition on Wnt and its inhibitors were analyzed using western blot and real-time quantitative PCR. The results showed that SMSP positively regulated Wnt/β-catenin signaling by increasing the expression of β-catenin and p-GSK3β protein, which resulted from the weakened expression of the Wnt inhibitor Dickkopf-1 (DKK1). On the contrary, L-733060 lowered the expression of β-catenin and p-GSK3β protein through the up-regulation of DKK1 expression. Furthermore, in L-733060-treated mice, it was found that the pigmentation level as well as the melanogenic proteins and β-catenin protein expression were down-regulated, while the expression of DKK1 was up-regulated. These results showed the interaction between NK-1R and Wnt in human melanocytes in vitro and C57BL/6J mice in vivo, indicating that NK-1R may positively regulate melanogenesis through Wnt/β-catenin signaling pathway.

Keywords: L-733060; Met(O2)11] substance P; Wnt/β-catenin; [Sar9; neurokinin-1 receptor.

MeSH terms

  • Animals
  • Cells, Cultured
  • Dose-Response Relationship, Drug
  • Glycogen Synthase Kinase 3 beta / metabolism
  • Humans
  • Intercellular Signaling Peptides and Proteins / genetics
  • Intercellular Signaling Peptides and Proteins / metabolism
  • Melanins / biosynthesis*
  • Melanocytes / drug effects
  • Melanocytes / metabolism*
  • Mice, Inbred C57BL
  • Neurokinin-1 Receptor Antagonists / pharmacology
  • Phosphorylation
  • Piperidines / pharmacology
  • Receptors, Neurokinin-1 / drug effects
  • Receptors, Neurokinin-1 / metabolism*
  • Skin / cytology
  • Skin / drug effects
  • Skin / metabolism*
  • Skin Pigmentation* / drug effects
  • Substance P / analogs & derivatives
  • Substance P / pharmacology
  • Time Factors
  • Wnt Signaling Pathway* / drug effects
  • beta Catenin / genetics
  • beta Catenin / metabolism*

Substances

  • CTNNB1 protein, human
  • CTNNB1 protein, mouse
  • DKK1 protein, human
  • Dkk1 protein, mouse
  • Intercellular Signaling Peptides and Proteins
  • Melanins
  • Neurokinin-1 Receptor Antagonists
  • Piperidines
  • Receptors, Neurokinin-1
  • beta Catenin
  • substance P, Sar(9)-Met(O2)(11)-
  • 3-((3,5-bis(trifluoromethyl)phenyl)methyloxy)-2-phenylpiperidine
  • Substance P
  • GSK3B protein, human
  • Glycogen Synthase Kinase 3 beta
  • Gsk3b protein, mouse