Mutant V600E BRAF increases hypoxia inducible factor-1alpha expression in melanoma

Cancer Res. 2007 Apr 1;67(7):3177-84. doi: 10.1158/0008-5472.CAN-06-3312.

Abstract

Mutations in the BRAF serine/threonine kinase gene are frequently found in cutaneous melanomas. Activation of hypoxia inducible factor-1alpha (HIF-1alpha) in response to both hypoxic stress and oncogenic signals has important implications in cancer development and progression. Here, we report that mutant BRAF(V600E) increases HIF-1alpha expression in melanoma cells. Our microarray profiling data in 35 melanoma and melanocyte cell lines showed that HIF-1alpha gene expression was significantly increased in melanomas harboring BRAF(V600E) mutation. Stable suppression of mutant BRAF(V600E) or both wild-type and mutant BRAF(V600E) by RNA interference in melanoma cells resulted in significantly decreased HIF-1alpha expression. Knockdown of mutant BRAF(V600E) induced significant reduction of cell survival and proliferation under hypoxic conditions, whereas knockdown of both wild-type and mutant BRAF(V600E) resulted in further reduction. The effects of BRAF knockdown can be rescued by reintroducing BRAF(V600E) into tumor cells. Transfection of BRAF(V600E) into melanoma cells with wild-type BRAF induced significantly more hypoxic tolerance. Knockdown of HIF-1alpha in melanoma cells resulted in decreased cell survival under hypoxic conditions. Pharmacologic inhibition of BRAF by BAY 43-9006 also resulted in decreased HIF-1alpha expression. Although HIF-1alpha translational rate was not changed, the protein was less stable in BRAF knockdown cells. In additional, von Hippel-Lindau protein expression was significantly increased in BRAF knockdown cells. Our data show for the first time that BRAF(V600E) mutation increases HIF-1alpha expression and melanoma cell survival under hypoxic conditions and suggest that effects of the oncogenic V600E BRAF mutation may be partially mediated through the HIF-1alpha pathway.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Benzenesulfonates / pharmacology
  • Cell Hypoxia / physiology
  • Cell Line, Tumor
  • Cell Survival / physiology
  • Gene Expression Profiling
  • Gene Expression Regulation, Neoplastic
  • Humans
  • Hypoxia-Inducible Factor 1, alpha Subunit / antagonists & inhibitors
  • Hypoxia-Inducible Factor 1, alpha Subunit / biosynthesis*
  • Hypoxia-Inducible Factor 1, alpha Subunit / genetics
  • Hypoxia-Inducible Factor 1, alpha Subunit / metabolism
  • Melanoma / enzymology*
  • Melanoma / genetics
  • Melanoma / pathology
  • Mutation*
  • Niacinamide / analogs & derivatives
  • Phenylurea Compounds
  • Proto-Oncogene Proteins B-raf / genetics*
  • Pyridines / pharmacology
  • RNA Interference
  • RNA, Small Interfering / genetics
  • Sorafenib
  • Transfection
  • Up-Regulation

Substances

  • Benzenesulfonates
  • Hypoxia-Inducible Factor 1, alpha Subunit
  • Phenylurea Compounds
  • Pyridines
  • RNA, Small Interfering
  • Niacinamide
  • Sorafenib
  • BRAF protein, human
  • Proto-Oncogene Proteins B-raf