Phosphorylation by protein kinase A disassembles the caspase-9 core

Cell Death Differ. 2018 Jun;25(6):1025-1039. doi: 10.1038/s41418-017-0052-9. Epub 2018 Jan 19.

Abstract

Caspases, the cysteine proteases which facilitate the faithful execution of apoptosis, are tightly regulated by a number of mechanisms including phosphorylation. In response to cAMP, PKA phosphorylates caspase-9 at three sites preventing caspase-9 activation, and suppressing apoptosis progression. Phosphorylation of caspase-9 by PKA at the functionally relevant site Ser-183 acts as an upstream block of the apoptotic cascade, directly inactivating caspase-9 by a two-stage mechanism. First, Ser-183 phosphorylation prevents caspase-9 self-processing and directly blocks substrate binding. In addition, Ser-183 phosphorylation breaks the fundamental interactions within the caspase-9 core, promoting disassembly of the large and small subunits. This occurs despite Ser-183 being a surface residue distal from the interface between the large and small subunits. This phosphorylation-induced disassembly promotes the formation of ordered aggregates around 20 nm in diameter. Similar aggregates of caspase-9 have not been previously reported. This two-stage regulatory mechanism for caspase-9 has likewise not been reported previously but may be conserved across the caspases.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Caspase 3 / chemistry*
  • Caspase 3 / genetics
  • Caspase 3 / metabolism
  • Caspase 9 / chemistry*
  • Caspase 9 / genetics
  • Caspase 9 / metabolism
  • Cyclic AMP-Dependent Protein Kinases / chemistry*
  • Cyclic AMP-Dependent Protein Kinases / genetics
  • Cyclic AMP-Dependent Protein Kinases / metabolism
  • Humans
  • Phosphorylation

Substances

  • Cyclic AMP-Dependent Protein Kinases
  • CASP3 protein, human
  • CASP9 protein, human
  • Caspase 3
  • Caspase 9