Inhibition of hypoxia-inducible factor-1 function enhances the sensitivity of multiple myeloma cells to melphalan

Mol Cancer Ther. 2009 Aug;8(8):2329-38. doi: 10.1158/1535-7163.MCT-09-0150. Epub 2009 Aug 11.

Abstract

Abnormal activation of hypoxia-inducible factor-1 (HIF-1), one of the most important transcription factors for the adaptation of cells to hypoxia, is frequently observed in numerous types of solid tumors. Dysregulation of HIF-1 induces tumor angiogenesis and enhances the expression of anti-apoptotic proteins and glycolysis-associated enzymes in cancer cells, which in turn leads to the promotion of tumor growth. In the present study, we examined the pathophysiologic role of HIF-1 in multiple myeloma. Furthermore, we explored the possibility that HIF-1 may be a molecular target for myeloma therapy. We identified constitutive expression of the hypoxia-inducible factor-1 alpha (HIF-1alpha)-subunit in established myeloma cell lines and in primary myeloma cells. Treatment with insulin-like growth factor-1 (IGF-1) significantly increased HIF-1alpha expression through activation of the AKT and mitogen-activated protein kinase signaling pathways. Inhibition of HIF-1 function either by echinomycin, a specific HIF-1 inhibitor, or a siRNA against HIF-1alpha resulted in enhanced sensitivity to melphalan in myeloma cells. This inhibition of HIF-1 also reversed the protective effect of IGF-1 on melphalan-induced apoptosis. Inhibition of HIF-1 drastically reduced both basal and IGF-1-induced expression of survivin, one of the most important anti-apoptotic proteins in myeloma cells. We conclude that HIF-1 inhibition may be an attractive therapeutic strategy for multiple myeloma.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antigens, CD19 / metabolism
  • Antineoplastic Agents, Alkylating / pharmacology*
  • Apoptosis
  • Cell Line, Tumor
  • Echinomycin / pharmacology
  • Fluorescent Antibody Technique
  • Humans
  • Hypoxia-Inducible Factor 1 / antagonists & inhibitors*
  • Hypoxia-Inducible Factor 1 / metabolism
  • Insulin-Like Growth Factor I / metabolism
  • Melphalan / pharmacology*
  • Mitogen-Activated Protein Kinases / metabolism
  • Multiple Myeloma / drug therapy*
  • Multiple Myeloma / metabolism
  • Phosphatidylinositol 3-Kinases / metabolism
  • RNA, Small Interfering / metabolism

Substances

  • Antigens, CD19
  • Antineoplastic Agents, Alkylating
  • Hypoxia-Inducible Factor 1
  • RNA, Small Interfering
  • Echinomycin
  • Insulin-Like Growth Factor I
  • Phosphatidylinositol 3-Kinases
  • Mitogen-Activated Protein Kinases
  • Melphalan