CDK9-mediated transcription elongation is required for MYC addiction in hepatocellular carcinoma

Genes Dev. 2014 Aug 15;28(16):1800-14. doi: 10.1101/gad.244368.114.

Abstract

One-year survival rates for newly diagnosed hepatocellular carcinoma (HCC) are <50%, and unresectable HCC carries a dismal prognosis owing to its aggressiveness and the undruggable nature of its main genetic drivers. By screening a custom library of shRNAs directed toward known drug targets in a genetically defined Myc-driven HCC model, we identified cyclin-dependent kinase 9 (Cdk9) as required for disease maintenance. Pharmacological or shRNA-mediated CDK9 inhibition led to robust anti-tumor effects that correlated with MYC expression levels and depended on the role that both CDK9 and MYC exert in transcription elongation. Our results establish CDK9 inhibition as a therapeutic strategy for MYC-overexpressing liver tumors and highlight the relevance of transcription elongation in the addiction of cancer cells to MYC.

Keywords: CDK9; MYC; RNAi screen; oncogene addiction; transcription elongation.

Publication types

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

MeSH terms

  • Animals
  • Carcinoma, Hepatocellular / enzymology*
  • Carcinoma, Hepatocellular / genetics
  • Carcinoma, Hepatocellular / pathology
  • Cell Line, Tumor
  • Cell Proliferation
  • Cyclin-Dependent Kinase 9 / metabolism*
  • Female
  • Gene Expression
  • Gene Library
  • Hep G2 Cells
  • Humans
  • Liver Neoplasms / enzymology*
  • Liver Neoplasms / genetics
  • Liver Neoplasms / pathology
  • Mice
  • Positive Transcriptional Elongation Factor B / genetics
  • Positive Transcriptional Elongation Factor B / metabolism
  • Proto-Oncogene Proteins c-myc / genetics
  • Proto-Oncogene Proteins c-myc / metabolism*
  • RNA Interference
  • RNA, Small Interfering / metabolism
  • Transcription Elongation, Genetic / physiology*

Substances

  • Myc protein, mouse
  • Proto-Oncogene Proteins c-myc
  • RNA, Small Interfering
  • Positive Transcriptional Elongation Factor B
  • Cyclin-Dependent Kinase 9