Targeting of MCL-1 kills MYC-driven mouse and human lymphomas even when they bear mutations in p53

Genes Dev. 2014 Jan 1;28(1):58-70. doi: 10.1101/gad.232009.113.

Abstract

The transcriptional regulator c-MYC is abnormally overexpressed in many human cancers. Evasion from apoptosis is critical for cancer development, particularly c-MYC-driven cancers. We explored which anti-apoptotic BCL-2 family member (expressed under endogenous regulation) is essential to sustain c-MYC-driven lymphoma growth to reveal which should be targeted for cancer therapy. Remarkably, inducible Cre-mediated deletion of even a single Mcl-1 allele substantially impaired the growth of c-MYC-driven mouse lymphomas. Mutations in p53 could diminish but not obviate the dependency of c-MYC-driven mouse lymphomas on MCL-1. Importantly, targeting of MCL-1 killed c-MYC-driven human Burkitt lymphoma cells, even those bearing mutations in p53. Given that loss of one allele of Mcl-1 is well tolerated in healthy tissues, our results suggest that therapeutic targeting of MCL-1 would be an attractive therapeutic strategy for MYC-driven cancers.

Keywords: BCL-2; MCL-1; MYC; apoptosis; cancer; p53.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Cell Proliferation
  • Cell Survival / genetics
  • Gene Expression Regulation, Neoplastic
  • Humans
  • Lymphoma / genetics*
  • Lymphoma / pathology
  • Lymphoma / therapy*
  • Mice
  • Mice, Inbred C57BL
  • Mutation*
  • Myeloid Cell Leukemia Sequence 1 Protein / genetics*
  • Protein Binding
  • Proto-Oncogene Proteins c-myc / genetics
  • Proto-Oncogene Proteins c-myc / metabolism*
  • Tumor Suppressor Protein p53 / genetics*

Substances

  • Myeloid Cell Leukemia Sequence 1 Protein
  • Proto-Oncogene Proteins c-myc
  • Tumor Suppressor Protein p53