p85β regulates autophagic degradation of AXL to activate oncogenic signaling

Nat Commun. 2020 May 8;11(1):2291. doi: 10.1038/s41467-020-16061-7.

Abstract

PIK3R2 encodes the p85β regulatory subunit of phosphatidylinositol 3-kinase and is frequently amplified in cancers. The signaling mechanism and therapeutic implication of p85β are poorly understood. Here we report that p85β upregulates the protein level of the receptor tyrosine kinase AXL to induce oncogenic signaling in ovarian cancer. p85β activates p110 activity and AKT-independent PDK1/SGK3 signaling to promote tumorigenic phenotypes, which are all abolished upon inhibition of AXL. At the molecular level, p85β alters the phosphorylation of TRIM2 (an E3 ligase) and optineurin (an autophagy receptor), which mediate the selective regulation of AXL by p85β, thereby disrupting the autophagic degradation of the AXL protein. Therapeutically, p85β expression renders ovarian cancer cells vulnerable to inhibitors of AXL, p110, or PDK1. Conversely, p85β-depleted cells are less sensitive to these inhibitors. Together, our findings provide a rationale for pharmacological blockade of the AXL signaling axis in PIK3R2-amplified ovarian cancer.

Publication types

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

MeSH terms

  • Autophagy*
  • Axl Receptor Tyrosine Kinase
  • Carcinogenesis / metabolism*
  • Cell Cycle Proteins / metabolism
  • Cell Line, Tumor
  • Class Ia Phosphatidylinositol 3-Kinase / metabolism*
  • Disease-Free Survival
  • Enzyme Activation
  • Female
  • Gene Ontology
  • Humans
  • Lysosomes / metabolism
  • Membrane Transport Proteins / metabolism
  • Nuclear Proteins
  • Ovarian Neoplasms / pathology
  • Phosphorylation
  • Proteolysis*
  • Proto-Oncogene Proteins / metabolism*
  • Proto-Oncogene Proteins c-akt / metabolism
  • Receptor Protein-Tyrosine Kinases / metabolism*
  • Signal Transduction*
  • Ubiquitination
  • Up-Regulation / genetics

Substances

  • Cell Cycle Proteins
  • Membrane Transport Proteins
  • NARF protein, human
  • Nuclear Proteins
  • OPTN protein, human
  • Proto-Oncogene Proteins
  • Class Ia Phosphatidylinositol 3-Kinase
  • Receptor Protein-Tyrosine Kinases
  • Proto-Oncogene Proteins c-akt
  • Axl Receptor Tyrosine Kinase
  • AXL protein, human