Inhibition of cGMP-dependent protein kinases potently decreases neutrophil spontaneous apoptosis

Biochem Biophys Res Commun. 2002 Sep 27;297(3):498-501. doi: 10.1016/s0006-291x(02)02246-5.

Abstract

The signalling pathways mediating neutrophil spontaneous apoptosis are still largely unknown. We report that the indolocarbazole compound KT5823, a specific inhibitor of cGMP-dependent protein kinases (cGK), dose-dependently inhibited spontaneous apoptosis of neutrophils. At the concentration eliciting the maximum effect (8 microM), it decreased apoptosis from 72.42+/-12.79% to 45.86+/-7.22% (p=0.0002, n=6). Similarly, the isoquinoline sulfonamide compound H89, another cGK inhibitor, prevented neutrophil apoptosis. At the concentration eliciting the maximum effect (20 microM), it decreased apoptosis from 72.42+/-12.79% to 31.84+/-10.70% (p=0.0004, n=6). The maximum effect of KT5823 and H89 was comparable to that of GM-CSF and LPS, respectively. Moreover, YC-1, a soluble guanylate cyclase activator, and 4-([3',4',-(methylenedioxy)benzyl]amino)-6-methoxyquinazoline, a specific phosphodiesterase 5 inhibitor, enhanced neutrophil apoptosis, and their effect was antagonised by KT5823. Taken together, these observations highlight a new role of cGK as important mediators of neutrophil spontaneous apoptosis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkaloids / pharmacology
  • Apoptosis / drug effects
  • Apoptosis / physiology*
  • Carbazoles*
  • Cells, Cultured
  • Cyclic GMP-Dependent Protein Kinases / antagonists & inhibitors*
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Indoles*
  • Isoquinolines / pharmacology
  • Kinetics
  • Neutrophils / cytology
  • Neutrophils / enzymology
  • Neutrophils / physiology*
  • Phosphodiesterase Inhibitors / pharmacology
  • Sulfonamides*

Substances

  • Alkaloids
  • Carbazoles
  • Enzyme Inhibitors
  • Indoles
  • Isoquinolines
  • Phosphodiesterase Inhibitors
  • Sulfonamides
  • KT 5823
  • Cyclic GMP-Dependent Protein Kinases
  • N-(2-(4-bromocinnamylamino)ethyl)-5-isoquinolinesulfonamide