SIRT1 promotes N-Myc oncogenesis through a positive feedback loop involving the effects of MKP3 and ERK on N-Myc protein stability

PLoS Genet. 2011 Jun;7(6):e1002135. doi: 10.1371/journal.pgen.1002135. Epub 2011 Jun 16.

Abstract

The N-Myc oncoprotein is a critical factor in neuroblastoma tumorigenesis which requires additional mechanisms converting a low-level to a high-level N-Myc expression. N-Myc protein is stabilized when phosphorylated at Serine 62 by phosphorylated ERK protein. Here we describe a novel positive feedback loop whereby N-Myc directly induced the transcription of the class III histone deacetylase SIRT1, which in turn increased N-Myc protein stability. SIRT1 binds to Myc Box I domain of N-Myc protein to form a novel transcriptional repressor complex at gene promoter of mitogen-activated protein kinase phosphatase 3 (MKP3), leading to transcriptional repression of MKP3, ERK protein phosphorylation, N-Myc protein phosphorylation at Serine 62, and N-Myc protein stabilization. Importantly, SIRT1 was up-regulated, MKP3 down-regulated, in pre-cancerous cells, and preventative treatment with the SIRT1 inhibitor Cambinol reduced tumorigenesis in TH-MYCN transgenic mice. Our data demonstrate the important roles of SIRT1 in N-Myc oncogenesis and SIRT1 inhibitors in the prevention and therapy of N-Myc-induced neuroblastoma.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Binding Sites / genetics
  • Cell Line, Tumor
  • Cell Proliferation
  • Dual Specificity Phosphatase 6 / genetics
  • Dual Specificity Phosphatase 6 / metabolism*
  • Enzyme Inhibitors / pharmacology
  • Extracellular Signal-Regulated MAP Kinases / metabolism*
  • Feedback, Physiological
  • Gene Expression Regulation, Neoplastic
  • Mice
  • Mice, Transgenic
  • Naphthalenes / pharmacology
  • Neuroblastoma / genetics
  • Neuroblastoma / metabolism
  • Neuroblastoma / pathology
  • Phosphorylation
  • Promoter Regions, Genetic
  • Protein Stability
  • Proto-Oncogene Proteins c-myc / genetics
  • Proto-Oncogene Proteins c-myc / metabolism*
  • Pyrimidinones / pharmacology
  • Random Allocation
  • Sirtuin 1 / genetics
  • Sirtuin 1 / metabolism*
  • Sp1 Transcription Factor / metabolism
  • Tumor Burden / drug effects
  • Tumor Burden / genetics

Substances

  • Enzyme Inhibitors
  • Naphthalenes
  • Proto-Oncogene Proteins c-myc
  • Pyrimidinones
  • Sp1 Transcription Factor
  • cambinol
  • Extracellular Signal-Regulated MAP Kinases
  • Dual Specificity Phosphatase 6
  • Sirt1 protein, mouse
  • Sirtuin 1