A Novel Serpin Regulatory Mechanism: SerpinB9 IS REVERSIBLY INHIBITED BY VICINAL DISULFIDE BOND FORMATION IN THE REACTIVE CENTER LOOP

J Biol Chem. 2016 Feb 12;291(7):3626-38. doi: 10.1074/jbc.M115.699298. Epub 2015 Dec 15.

Abstract

The intracellular protease inhibitor Sb9 (SerpinB9) is a regulator of the cytotoxic lymphocyte protease GzmB (granzyme B). Although GzmB is primarily involved in the destruction of compromised cells, recent evidence suggests that it is also involved in lysosome-mediated death of the cytotoxic lymphocyte itself. Sb9 protects the cell from GzmB released from lysosomes into the cytosol. Here we show that reactive oxygen species (ROS) generated within cytotoxic lymphocytes by receptor stimulation are required for lyososomal permeabilization and release of GzmB into the cytosol. Importantly, ROS also inactivate Sb9 by oxidizing a highly conserved cysteine pair (P1-P1' in rodents and P1'-P2' in other mammals) in the reactive center loop to form a vicinal disulfide bond. Replacement of the P4-P3' reactive center loop residues of the prototype serpin, SERPINA1, with the P4-P5' residues of Sb9 containing the cysteine pair is sufficient to convert SERPINA1 into a ROS-sensitive GzmB inhibitor. Conversion of the cysteine pair to serines in either human or mouse Sb9 results in a functional serpin that inhibits GzmB and resists ROS inactivation. We conclude that ROS sensitivity of Sb9 allows the threshold for GzmB-mediated suicide to be lowered, as part of a conserved post-translational homeostatic mechanism regulating lymphocyte numbers or activity. It follows, for example, that antioxidants may improve NK cell viability in adoptive immunotherapy applications by stabilizing Sb9.

Keywords: SerpinB9; T cell; granzyme B; immunotherapy; lysosomal membrane permeabilization; lysosome; natural killer cells (NK cells); protease; reactive oxygen species (ROS); serpin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apoptosis
  • CD8-Positive T-Lymphocytes / cytology
  • CD8-Positive T-Lymphocytes / immunology
  • CD8-Positive T-Lymphocytes / metabolism*
  • Cell Line
  • Cells, Cultured
  • Cystine / chemistry
  • Granzymes / antagonists & inhibitors
  • Granzymes / chemistry
  • Granzymes / genetics
  • Granzymes / metabolism*
  • Humans
  • Jurkat Cells
  • Killer Cells, Natural / cytology
  • Killer Cells, Natural / immunology
  • Killer Cells, Natural / metabolism*
  • Lysosomes / enzymology
  • Lysosomes / metabolism
  • Membrane Proteins / antagonists & inhibitors
  • Membrane Proteins / chemistry
  • Membrane Proteins / genetics
  • Membrane Proteins / metabolism*
  • Mice
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Mutant Proteins
  • Peptide Fragments / chemistry
  • Peptide Fragments / genetics
  • Peptide Fragments / metabolism
  • Reactive Oxygen Species / metabolism*
  • Recombinant Fusion Proteins / chemistry
  • Recombinant Fusion Proteins / metabolism
  • Recombinant Proteins / chemistry
  • Recombinant Proteins / metabolism
  • Serpins / chemistry
  • Serpins / genetics
  • Serpins / metabolism*

Substances

  • Membrane Proteins
  • Mutant Proteins
  • Peptide Fragments
  • Reactive Oxygen Species
  • Recombinant Fusion Proteins
  • Recombinant Proteins
  • SERPINB9 protein, human
  • Serpins
  • Cystine
  • GZMB protein, human
  • Granzymes
  • Gzmb protein, mouse
  • Serpinb9 protein, mouse