IL-converting enzyme/caspase-1 inhibitor VX-765 blocks the hypersensitive response to an inflammatory stimulus in monocytes from familial cold autoinflammatory syndrome patients

J Immunol. 2005 Aug 15;175(4):2630-4. doi: 10.4049/jimmunol.175.4.2630.

Abstract

Familial cold autoinflammatory syndrome (FCAS) and the related autoinflammatory disorders, Muckle-Wells syndrome and neonatal onset multisystem inflammatory disease, are characterized by mutations in the CIAS1 gene that encodes cryopyrin, an adaptor protein involved in activation of IL-converting enzyme/caspase-1. Mutations in cryopyrin are hypothesized to result in abnormal secretion of caspase-1-dependent proinflammatory cytokines, IL-1beta and IL-18. In this study, we examined cytokine secretion in PBMCs from FCAS patients and found a marked hyperresponsiveness of both IL-1beta and IL-18 secretion to LPS stimulation, but no evidence of increased basal secretion of these cytokines, or alterations in basal or stimulated pro-IL-1beta levels. VX-765, an orally active IL-converting enzyme/caspase-1 inhibitor, blocked IL-1beta secretion with equal potency in LPS-stimulated cells from FCAS and control subjects. These results further link mutations in cryopyrin with abnormal caspase-1 activation, and support the clinical testing of caspase-1 inhibitors such as VX-765 in autoinflammatory disorders.

Publication types

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

MeSH terms

  • Adult
  • Aged
  • Aged, 80 and over
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Autoimmune Diseases / enzymology
  • Autoimmune Diseases / genetics
  • Autoimmune Diseases / immunology*
  • Carrier Proteins / genetics
  • Carrier Proteins / physiology
  • Caspase 1 / biosynthesis
  • Caspase 1 / physiology
  • Caspase Inhibitors*
  • Cold Temperature / adverse effects*
  • Cysteine Proteinase Inhibitors / pharmacology*
  • Cytokines / metabolism
  • Drug Evaluation, Preclinical
  • Female
  • Humans
  • Hypersensitivity / enzymology
  • Hypersensitivity / genetics
  • Hypersensitivity / immunology
  • Hypersensitivity / prevention & control*
  • Inflammation / enzymology
  • Inflammation / genetics
  • Inflammation / prevention & control
  • Interleukin-1 / antagonists & inhibitors
  • Interleukin-1 / biosynthesis
  • Interleukin-1 / metabolism
  • Lipopolysaccharides / pharmacology
  • Male
  • Middle Aged
  • Monocytes / enzymology
  • Monocytes / metabolism
  • Monocytes / pathology*
  • NLR Family, Pyrin Domain-Containing 3 Protein
  • Prodrugs / pharmacology
  • Protein Precursors / biosynthesis
  • Syndrome

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Carrier Proteins
  • Caspase Inhibitors
  • Cysteine Proteinase Inhibitors
  • Cytokines
  • Interleukin-1
  • Lipopolysaccharides
  • NLR Family, Pyrin Domain-Containing 3 Protein
  • NLRP3 protein, human
  • Prodrugs
  • Protein Precursors
  • Caspase 1