Genetic and pharmacologic inhibition of β-catenin targets imatinib-resistant leukemia stem cells in CML

Cell Stem Cell. 2012 Apr 6;10(4):412-24. doi: 10.1016/j.stem.2012.02.017.

Abstract

A key characteristic of hematopoietic stem cells (HSCs) is the ability to self-renew. Genetic deletion of β-catenin during fetal HSC development leads to impairment of self-renewal while β-catenin is dispensable in fully developed adult HSCs. Whether β-catenin is required for maintenance of fully developed CML leukemia stem cells (LSCs) is unknown. Here, we use a conditional mouse model to show that deletion of β-catenin after CML initiation does not lead to a significant increase in survival. However, deletion of β-catenin synergizes with imatinib (IM) to delay disease recurrence after imatinib discontinuation and to abrogate CML stem cells. These effects can be mimicked by pharmacologic inhibition of β-catenin via modulation of prostaglandin signaling. Treatment with the cyclooxygenase inhibitor indomethacin reduces β-catenin levels and leads to a reduction in LSCs. In conclusion, inhibiting β-catenin by genetic inactivation or pharmacologic modulation is an effective combination therapy with imatinib and targets CML stem cells.

Publication types

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

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Benzamides
  • Cyclooxygenase Inhibitors / pharmacology*
  • Drug Resistance, Neoplasm / drug effects*
  • Drug Resistance, Neoplasm / genetics*
  • Gene Deletion
  • Humans
  • Imatinib Mesylate
  • Indomethacin / pharmacology*
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive* / genetics
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive* / metabolism
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive* / pathology
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive* / therapy
  • Mice
  • Neoplastic Stem Cells / metabolism*
  • Neoplastic Stem Cells / pathology
  • Piperazines / pharmacology*
  • Prostaglandins / metabolism
  • Pyrimidines / pharmacology*
  • beta Catenin* / antagonists & inhibitors
  • beta Catenin* / genetics

Substances

  • Antineoplastic Agents
  • Benzamides
  • Cyclooxygenase Inhibitors
  • Piperazines
  • Prostaglandins
  • Pyrimidines
  • beta Catenin
  • Imatinib Mesylate
  • Indomethacin