Regulation of Tumor-Associated Myeloid Cell Activity by CBP/EP300 Bromodomain Modulation of H3K27 Acetylation

Cell Rep. 2019 Apr 2;27(1):269-281.e4. doi: 10.1016/j.celrep.2019.03.008.

Abstract

Myeloid-derived suppressor cells (MDSCs) are found in most cancer malignancies and support tumorigenesis by suppressing immunity and promoting tumor growth. Here we identify the bromodomain (BRD) of CBP/EP300 as a critical regulator of H3K27 acetylation (H3K27ac) in MDSCs across promoters and enhancers of pro-tumorigenic target genes. In preclinical tumor models, in vivo administration of a CBP/EP300-BRD inhibitor (CBP/EP300-BRDi) alters intratumoral MDSCs and attenuates established tumor growth in immunocompetent tumor-bearing mice, as well as in MDSC-dependent xenograft models. Inhibition of CBP/EP300-BRD redirects tumor-associated MDSCs from a suppressive to an inflammatory phenotype through downregulation of STAT pathway-related genes and inhibition of Arg1 and iNOS. Similarly, CBP/EP300-BRDi decreases differentiation and suppressive function of human MDSCs in vitro. Our findings uncover a role of CBP/EP300-BRD in intratumoral MDSCs that may be targeted therapeutically to boost anti-tumor immunity.

Keywords: CBP; EP300; H3K27ac; bromodomain; myeloid-derived suppressive cells; tumors.

MeSH terms

  • Acetylation
  • Animals
  • Arginase / genetics
  • Arginase / metabolism
  • Carcinogenesis / metabolism*
  • Cell Line, Tumor
  • Cells, Cultured
  • Enhancer Elements, Genetic
  • Histones / metabolism*
  • Humans
  • Mice
  • Mice, Inbred BALB C
  • Mice, SCID
  • Myeloid Cells / metabolism*
  • Nitric Oxide Synthase Type II / genetics
  • Nitric Oxide Synthase Type II / metabolism
  • Promoter Regions, Genetic
  • Protein Domains
  • STAT Transcription Factors / metabolism
  • p300-CBP Transcription Factors / chemistry
  • p300-CBP Transcription Factors / metabolism*

Substances

  • Histones
  • STAT Transcription Factors
  • Nitric Oxide Synthase Type II
  • p300-CBP Transcription Factors
  • Arg1 protein, mouse
  • Arginase