Heat shock protein 90 regulates the expression of Wilms tumor 1 protein in myeloid leukemias

Blood. 2010 Nov 25;116(22):4591-9. doi: 10.1182/blood-2009-10-247239. Epub 2010 Jul 22.

Abstract

The aberrant overexpression of Wilms tumor 1 (WT1) in myeloid leukemia plays an important role in blast cell survival and resistance to chemotherapy. High expression of WT1 is also associated with relapse and shortened disease-free survival in patients. However, the mechanisms by which WT1 expression is regulated in leukemia remain unclear. Here, we report that heat shock protein 90 (Hsp90), which plays a critical role in the folding and maturation of several oncogenic proteins, associates with WT1 protein and stabilizes its expression. Pharmacologic inhibition of Hsp90 resulted in ubiquitination and subsequent proteasome-dependant degradation of WT1. RNAi-mediated silencing of WT1 reduced the survival of leukemia cells and increased the sensitivity of these cells to chemotherapy and Hsp90 inhibition. Furthermore, Hsp90 inhibitors 17-AAG [17-(allylamino)-17-demethoxygeldanamycin] and STA-9090 significantly reduced the growth of myeloid leukemia xenografts in vivo and effectively down-regulated the expression of WT1 and its downstream target proteins, c-Myc and Bcl-2. Collectively, our studies identify WT1 as a novel Hsp90 client and support the crucial role for the WT1-Hsp90 interaction in maintaining leukemia cell survival. These findings have significant implications for developing effective therapies for myeloid leukemias and offer a strategy to inhibit the oncogenic functions of WT1 by clinically available Hsp90 inhibitors.

Publication types

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

MeSH terms

  • Animals
  • Antineoplastic Agents, Phytogenic / pharmacology
  • Apoptosis / drug effects
  • Benzoquinones / pharmacology
  • Benzoquinones / therapeutic use
  • Cell Line, Tumor
  • Etoposide / pharmacology
  • Female
  • Gene Expression Regulation, Leukemic*
  • Gene Silencing
  • HSP90 Heat-Shock Proteins / antagonists & inhibitors
  • HSP90 Heat-Shock Proteins / chemistry
  • HSP90 Heat-Shock Proteins / metabolism*
  • Humans
  • Lactams, Macrocyclic / pharmacology
  • Lactams, Macrocyclic / therapeutic use
  • Leukemia, Myeloid / drug therapy
  • Leukemia, Myeloid / genetics*
  • Leukemia, Myeloid / metabolism
  • Mice
  • Mice, SCID
  • Proteasome Endopeptidase Complex / metabolism
  • Protein Interaction Domains and Motifs
  • Protein Structure, Tertiary
  • Triazoles / therapeutic use
  • WT1 Proteins / chemistry
  • WT1 Proteins / genetics*
  • WT1 Proteins / metabolism

Substances

  • Antineoplastic Agents, Phytogenic
  • Benzoquinones
  • HSP90 Heat-Shock Proteins
  • Lactams, Macrocyclic
  • STA 9090
  • Triazoles
  • WT1 Proteins
  • tanespimycin
  • Etoposide
  • Proteasome Endopeptidase Complex