AKT-dependent phosphorylation of the adenosine deaminases ADAR-1 and -2 inhibits deaminase activity

Alberto Bavelloni1, Enrico Focaccia1,2, Manuela Piazzi1,2

  • 1IRCSS Istituto Ortopedico Rizzoli (IOR), Bologna, Italy.

Insights

The study reveals that AKT kinases phosphorylate nuclear RNA editing enzymes ADAR1 and ADAR2, inhibiting their activity. This AKT-dependent phosphorylation directly impacts RNA editing processes in cells.

Area of Science:

  • Molecular Biology
  • Biochemistry
  • Cell Biology

Background:

  • Nuclear substrates of AKT (a.k.a. murine thymoma viral oncogene homolog kinases) are poorly understood.
  • AKT kinases regulate crucial cellular processes through phosphorylation of cytosolic substrates.

Purpose of the Study:

  • To investigate the role of nuclear AKT substrates.
  • To identify and characterize the interaction between AKT kinases and nuclear RNA editing enzymes.

Main Methods:

  • Isolation and identification of nuclear AKT substrates from leukemic cell lines using mass spectrometry.
  • Coimmunoprecipitation and in vitro kinase assays to confirm AKT interaction and phosphorylation of ADAR1 and ADAR2.
  • Site-directed mutagenesis to identify specific phosphorylation sites and assess the impact on enzyme activity.

Main Results:

  • ADAR1 (p110 isoform) and ADAR2 were identified as nuclear AKT substrates.
  • AKT-1, -2, and -3 were shown to interact with and phosphorylate ADAR1 and ADAR2 at specific threonine residues (T738 for ADAR1, T553 for ADAR2).
  • Phosphomimic mutations at these sites significantly reduced ADAR1 and ADAR2 deaminase activity, indicating inhibition.

Conclusions:

  • AKT-dependent phosphorylation directly inhibits the enzymatic activity of ADAR1 and ADAR2.
  • Activation of AKT kinases has a significant impact on RNA editing.
  • This finding sheds light on the nuclear functions of AKT and its role in regulating gene expression post-transcriptionally.

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