Reversal of Imatinib resistance in BCR-ABL-positive leukemia after inhibition of the Na+/H+ exchanger

Cancer Lett. 2011 Sep 1;308(1):81-90. doi: 10.1016/j.canlet.2011.04.016. Epub 2011 May 14.

Abstract

The present study was undertaken to estimate the therapeutic benefit to down-regulate the Na(+)/H(+) exchanger 1 (NHE1) for reversing chemoresistance of BCR-ABL-positive leukemia patient cells and cell lines. As a result, after treatment with specific NHE1 inhibitor Cariporide or high K(+) buffer to decrease intracellular pH (pH(i)), cells from relapsed patients exhibited decreased Pgp level, enhanced Rhodamine123 and drug accumulation, decreased colony-forming ability and the modulations of mitogen-activated protein kinases (MAPKs) activities. Furthermore, we used BCR-ABL-positive cell line K562 and its resistant counterparts K562/DOX and K562/G01 cell lines for further study. Together, these findings suggest that Pgp may be associated with the reversal of drug resistance in BCR-ABL-positive leukemia patients and cell lines by the inhibition of NHE1 though MAPK pathways.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Aged
  • Benzamides
  • Cell Line, Tumor
  • Child
  • Child, Preschool
  • Doxorubicin / pharmacology
  • Drug Resistance, Neoplasm
  • Drug Synergism
  • Female
  • Guanidines / pharmacology
  • Humans
  • Imatinib Mesylate
  • K562 Cells
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive / drug therapy*
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive / metabolism
  • Male
  • Middle Aged
  • Mitogen-Activated Protein Kinases / metabolism
  • Piperazines / pharmacology*
  • Pyrimidines / pharmacology*
  • Sodium-Hydrogen Exchangers / antagonists & inhibitors*
  • Sodium-Hydrogen Exchangers / metabolism
  • Sulfones / pharmacology
  • Young Adult

Substances

  • Benzamides
  • Guanidines
  • Piperazines
  • Pyrimidines
  • Sodium-Hydrogen Exchangers
  • Sulfones
  • cariporide
  • Doxorubicin
  • Imatinib Mesylate
  • Mitogen-Activated Protein Kinases