The LINK-A lncRNA interacts with PtdIns(3,4,5)P3 to hyperactivate AKT and confer resistance to AKT inhibitors

Nat Cell Biol. 2017 Mar;19(3):238-251. doi: 10.1038/ncb3473. Epub 2017 Feb 20.

Abstract

Phosphatidylinositol-3,4,5-trisphosphate (PtdIns(3,4,5)P3 or PIP3) mediates signalling pathways as a second messenger in response to extracellular signals. Although primordial functions of phospholipids and RNAs have been hypothesized in the 'RNA world', physiological RNA-phospholipid interactions and their involvement in essential cellular processes have remained a mystery. We explicate the contribution of lipid-binding long non-coding RNAs (lncRNAs) in cancer cells. Among them, long intergenic non-coding RNA for kinase activation (LINK-A) directly interacts with the AKT pleckstrin homology domain and PIP3 at the single-nucleotide level, facilitating AKT-PIP3 interaction and consequent enzymatic activation. LINK-A-dependent AKT hyperactivation leads to tumorigenesis and resistance to AKT inhibitors. Genomic deletions of the LINK-A PIP3-binding motif dramatically sensitized breast cancer cells to AKT inhibitors. Furthermore, meta-analysis showed the correlation between LINK-A expression and incidence of a single nucleotide polymorphism (rs12095274: A > G), AKT phosphorylation status, and poor outcomes for breast and lung cancer patients. PIP3-binding lncRNA modulates AKT activation with broad clinical implications.

Publication types

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

MeSH terms

  • Binding, Competitive / drug effects
  • Cell Line, Tumor
  • DNA Copy Number Variations / genetics
  • Drug Resistance, Neoplasm / drug effects*
  • Enzyme Activation / drug effects
  • Female
  • Humans
  • Lipids / chemistry
  • Mutation / genetics
  • Nucleic Acid Conformation
  • Phosphatidylinositol Phosphates / metabolism*
  • Phosphorylation / drug effects
  • Protein Kinase Inhibitors / pharmacology*
  • Proto-Oncogene Proteins c-akt / antagonists & inhibitors*
  • Proto-Oncogene Proteins c-akt / metabolism*
  • RNA, Long Noncoding / chemistry
  • RNA, Long Noncoding / metabolism*
  • Risk Factors
  • Triple Negative Breast Neoplasms / pathology

Substances

  • LINK-A long non-coding RNA, human
  • Lipids
  • Phosphatidylinositol Phosphates
  • Protein Kinase Inhibitors
  • RNA, Long Noncoding
  • phosphatidylinositol 3,4,5-triphosphate
  • Proto-Oncogene Proteins c-akt