Protease-activated receptor-1-induced calcium signaling in gingival fibroblasts is mediated by sarcoplasmic reticulum calcium release and extracellular calcium influx

Cell Signal. 2004 Jun;16(6):731-40. doi: 10.1016/j.cellsig.2003.11.008.

Abstract

Thrombin is a serine protease activated during injury and inflammation. Thrombin and other proteases generated by periodontal pathogens affect the behavior of periodontal cells via activation of protease-activated receptors (PARs). We noted that thrombin and PAR-1 agonist peptide stimulated intracellular calcium levels ([Ca2+]i) of gingival fibroblasts (GF). This increase of [Ca2+]i was inhibited by EGTA and verapamil. U73122 and neomycin inhibited thrombin- and PAR-1-induced [Ca2+]i. Furthermore, 2-APB (75-100 microM, inositol triphosphate [IP3] receptor antagonist), thapsigargin (1 microM), SKF-96365 (200 microM) and W7 (50 and 100 microM) also suppressed the PAR-1- and thrombin-induced [Ca2+]i. However, H7 (100, 200 microM) and ryanodine showed little effects. Blocking Ca2+ efflux from mitochondria by CGP37157 (50, 100 microM) inhibited both thrombin- and PAR-1-induced [Ca2+]i. Thrombin induced the IP3 production of GF within 30-seconds of exposure, which was inhibited by U73122. These results indicate that mitochondrial calcium efflux and calcium-calmodulin pathways are related to thrombin and PAR-1 induced [Ca2+]i in GF. Thrombin-induced [Ca2+]i of GF is mainly due to PAR-1 activation, extracellular calcium influx via L-type calcium channel, PLC activation, then IP3 binding to IP3 receptor in sarcoplasmic reticulum, which leads to intracellular calcium release and subsequently alters cell membrane capacitative calcium entry.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Boron Compounds / pharmacology
  • Calcium / metabolism
  • Calcium Channels, L-Type / drug effects
  • Calcium Signaling / drug effects
  • Calcium Signaling / physiology*
  • Cells, Cultured
  • Enzyme Inhibitors / pharmacology
  • Fibroblasts / physiology*
  • Gingiva / physiology*
  • Humans
  • Mitochondria / metabolism*
  • Neomycin / pharmacology
  • Receptor, PAR-1 / metabolism*
  • Ryanodine / pharmacology
  • Sarcoplasmic Reticulum
  • Sulfonamides / pharmacology
  • Thapsigargin / pharmacology
  • Thrombin / metabolism
  • Verapamil / pharmacology

Substances

  • Boron Compounds
  • Calcium Channels, L-Type
  • Enzyme Inhibitors
  • Receptor, PAR-1
  • Sulfonamides
  • Ryanodine
  • W 7
  • Thapsigargin
  • Verapamil
  • 2-aminoethoxydiphenyl borate
  • Thrombin
  • Neomycin
  • Calcium