p21 expression is induced by activation of nuclear nerve growth factor-induced Balpha (Nur77) in pancreatic cancer cells

Mol Cancer Res. 2009 Jul;7(7):1169-78. doi: 10.1158/1541-7786.MCR-08-0473. Epub 2009 Jul 7.

Abstract

1,1-Bis(3'-indolyl)-1-(p-anisyl)methane (DIM-C-pPhOCH3) activates the orphan receptor nerve growth factor-induced Balpha (Nur77) in cancer cells, and in this study, DIM-C-pPhOCH3 decreased Panc1 pancreatic cancer cell survival and arrested cells in G0-G1. These responses were accompanied by induction of the cyclin-dependent kinase inhibitor p21 in pancreatic cancer cells. Mechanistic studies showed that induction of p21 mRNA and protein by DIM-C-pPhOCH3 was Nur77 dependent but did not depend on Krüppel-like factor 4, which was also induced by DIM-C-pPhOCH3. Activation of p21 promoter constructs by DIM-C-pPhOCH3 required the GC-rich proximal region of the promoter, and results of RNA interference studies showed that Nur77-dependent activation of the p21 promoter involved interactions with Sp1 and Sp4 but not Sp3. Interactions of Nur77 with the p21 promoter in Panc1 cells treated with DIM-C-pPhOCH3 were also confirmed in chromatin immunoprecipitation assays. These data show that activation of nuclear Nur77 results in a novel pathway for induction of p21, which is independent of Nur77 response elements but dependent on Sp proteins bound to the GC-rich proximal region of the p21 promoter.

Publication types

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

MeSH terms

  • Anisoles / pharmacology*
  • Apoptosis / physiology
  • Cell Growth Processes / physiology
  • Cell Line, Tumor
  • Cyclin-Dependent Kinase Inhibitor p21 / biosynthesis*
  • Cyclin-Dependent Kinase Inhibitor p21 / genetics
  • Cyclin-Dependent Kinase Inhibitor p21 / metabolism
  • Data Interpretation, Statistical
  • Gene Expression Regulation, Neoplastic
  • Humans
  • Indoles / metabolism
  • Indoles / pharmacology*
  • Intercalating Agents / metabolism
  • Kruppel-Like Factor 4
  • Nuclear Receptor Subfamily 4, Group A, Member 1 / biosynthesis
  • Nuclear Receptor Subfamily 4, Group A, Member 1 / genetics
  • Nuclear Receptor Subfamily 4, Group A, Member 1 / metabolism*
  • Pancreatic Neoplasms / genetics
  • Pancreatic Neoplasms / metabolism*
  • Pancreatic Neoplasms / pathology
  • Promoter Regions, Genetic

Substances

  • 1,1-bis(3'-indolyl)-1-(p-anisyl)methane
  • Anisoles
  • CDKN1A protein, human
  • Cyclin-Dependent Kinase Inhibitor p21
  • Indoles
  • Intercalating Agents
  • KLF4 protein, human
  • Kruppel-Like Factor 4
  • NR4A1 protein, human
  • Nuclear Receptor Subfamily 4, Group A, Member 1
  • DAPI