A framework for identification of actionable cancer genome dependencies in small cell lung cancer

Proc Natl Acad Sci U S A. 2012 Oct 16;109(42):17034-9. doi: 10.1073/pnas.1207310109. Epub 2012 Oct 3.

Abstract

Small cell lung cancer (SCLC) accounts for about 15% of all lung cancers. The prognosis of SCLC patients is devastating and no biologically targeted therapeutics are active in this tumor type. To develop a framework for development of specific SCLC-targeted drugs we conducted a combined genomic and pharmacological vulnerability screen in SCLC cell lines. We show that SCLC cell lines capture the genomic landscape of primary SCLC tumors and provide genetic predictors for activity of clinically relevant inhibitors by screening 267 compounds across 44 of these cell lines. We show Aurora kinase inhibitors are effective in SCLC cell lines bearing MYC amplification, which occur in 3-7% of SCLC patients. In MYC-amplified SCLC cells Aurora kinase inhibition associates with G2/M-arrest, inactivation of PI3-kinase (PI3K) signaling, and induction of apoptosis. Aurora dependency in SCLC primarily involved Aurora B, required its kinase activity, and was independent of depletion of cytoplasmic levels of MYC. Our study suggests that a fraction of SCLC patients may benefit from therapeutic inhibition of Aurora B. Thus, thorough chemical and genomic exploration of SCLC cell lines may provide starting points for further development of rational targeted therapeutic intervention in this deadly tumor type.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Apoptosis / drug effects
  • Aurora Kinase B
  • Aurora Kinases
  • Benzothiazoles
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • DNA Primers / genetics
  • Diamines
  • Enzyme Inhibitors / pharmacology*
  • Flow Cytometry
  • G2 Phase Cell Cycle Checkpoints / drug effects
  • G2 Phase Cell Cycle Checkpoints / physiology*
  • Humans
  • Immunoblotting
  • Organic Chemicals
  • Phosphoinositide-3 Kinase Inhibitors
  • Protein Serine-Threonine Kinases / antagonists & inhibitors*
  • Proto-Oncogene Proteins c-myc / metabolism
  • Quinolines
  • Reverse Transcriptase Polymerase Chain Reaction
  • Signal Transduction / drug effects*
  • Small Cell Lung Carcinoma / drug therapy*
  • Small Cell Lung Carcinoma / genetics*

Substances

  • Benzothiazoles
  • DNA Primers
  • Diamines
  • Enzyme Inhibitors
  • MYC protein, human
  • Organic Chemicals
  • Phosphoinositide-3 Kinase Inhibitors
  • Proto-Oncogene Proteins c-myc
  • Quinolines
  • SYBR Green I
  • AURKB protein, human
  • Aurora Kinase B
  • Aurora Kinases
  • Protein Serine-Threonine Kinases

Associated data

  • GEO/GSE40142