Induced degradation of lineage-specific oncoproteins drives the therapeutic vulnerability of small cell lung cancer to PARP inhibitors

Sci Adv. 2024 Jan 19;10(3):eadh2579. doi: 10.1126/sciadv.adh2579. Epub 2024 Jan 19.

Abstract

Although BRCA1/2 mutations are not commonly found in small cell lung cancer (SCLC), a substantial fraction of SCLC shows clinically relevant response to PARP inhibitors (PARPis). However, the underlying mechanism(s) of PARPi sensitivity in SCLC is poorly understood. We performed quantitative proteomic analyses and identified proteomic changes that signify PARPi responses in SCLC cells. We found that the vulnerability of SCLC to PARPi could be explained by the degradation of lineage-specific oncoproteins (e.g., ASCL1). PARPi-induced activation of the E3 ligase HUWE1 mediated the ubiquitin-proteasome system (UPS)-dependent ASCL1 degradation. Although PARPi induced a general DNA damage response in SCLC cells, this signal generated a cell-specific response in ASCL1 degradation, leading to the identification of HUWE1 expression as a predictive biomarker for PARPi. Combining PARPi with agents targeting these pathways markedly improved therapeutic response in SCLC. The degradation of lineage-specific oncoproteins therefore represents a previously unidentified mechanism for PARPi efficacy in SCLC.

MeSH terms

  • BRCA1 Protein / genetics
  • BRCA2 Protein / genetics
  • Cell Line, Tumor
  • Humans
  • Lung Neoplasms* / drug therapy
  • Lung Neoplasms* / genetics
  • Lung Neoplasms* / metabolism
  • Oncogene Proteins
  • Poly(ADP-ribose) Polymerase Inhibitors / pharmacology
  • Proteomics
  • Small Cell Lung Carcinoma* / drug therapy
  • Small Cell Lung Carcinoma* / genetics
  • Small Cell Lung Carcinoma* / metabolism
  • Tumor Suppressor Proteins
  • Ubiquitin-Protein Ligases / genetics

Substances

  • BRCA1 protein, human
  • BRCA1 Protein
  • Poly(ADP-ribose) Polymerase Inhibitors
  • BRCA2 protein, human
  • BRCA2 Protein
  • Oncogene Proteins
  • HUWE1 protein, human
  • Tumor Suppressor Proteins
  • Ubiquitin-Protein Ligases