Therapeutic targeting of c-Myc in T-cell acute lymphoblastic leukemia, T-ALL

Oncotarget. 2014 May 30;5(10):3168-72. doi: 10.18632/oncotarget.1873.

Abstract

T-ALL patients treated with intensive chemotherapy achieve high rates of remission. However, frequent long-term toxicities and relapses into chemotherapy-refractory tumors constitute major clinical challenges which could be met by targeted therapies. c-MYC is a central oncogene in T-ALL, prompting the exploration of the efficacy of MYC inhibitors such as JQ1 (BET-bromodomain inhibitor), and SAHA (HDAC inhibitor). Using a standardized ex vivo drug screening assay, we show here that JQ1 and SAHA show competitive efficiency compared to inhibitors of proteasome, PI3K/AKT/mTOR and NOTCH pathways, and synergize in combination with Vincristine. We also compared for the first time the in vivo relevance of such associations in mice xenografted with human primary T-ALLs. Our data indicate that although treatments combining JQ1 or SAHA with chemotherapeutic regimens might represent promising developments in T-ALL, combinations will need to be tailored to specific subgroups of responsive patients, the profiles of which still remain to be precisely defined.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Combined Chemotherapy Protocols / pharmacology*
  • Azepines / administration & dosage
  • Drug Screening Assays, Antitumor
  • Drug Synergism
  • Histone Deacetylase Inhibitors / administration & dosage
  • Humans
  • Mice
  • Nylons
  • Precursor T-Cell Lymphoblastic Leukemia-Lymphoma / metabolism*
  • Proto-Oncogene Proteins c-myc / antagonists & inhibitors*
  • Pyrroles / administration & dosage
  • Triazoles / administration & dosage
  • Xenograft Model Antitumor Assays

Substances

  • (+)-JQ1 compound
  • Azepines
  • Histone Deacetylase Inhibitors
  • MYC protein, human
  • Nylons
  • Proto-Oncogene Proteins c-myc
  • Pyrroles
  • SAHA-PIP-delta
  • Triazoles