Inhibitors of Bcl-2 protein family deplete ER Ca2+ stores in pancreatic acinar cells

Pflugers Arch. 2010 Oct;460(5):891-900. doi: 10.1007/s00424-010-0859-4. Epub 2010 Jul 9.

Abstract

Physiological stimulation of pancreatic acinar cells by cholecystokinin and acetylcholine activate a spatial-temporal pattern of cytosolic [Ca(+2)] changes that are regulated by a coordinated response of inositol 1,4,5-trisphosphate receptors (IP(3)Rs), ryanodine receptors (RyRs) and calcium-induced calcium release (CICR). For the present study, we designed experiments to determine the potential role of Bcl-2 proteins in these patterns of cytosolic [Ca(+2)] responses. We used small molecule inhibitors that disrupt the interactions between prosurvival Bcl-2 proteins (i.e. Bcl-2 and Bcl-xl) and proapoptotic Bcl-2 proteins (i.e. Bax) and fluorescence microfluorimetry techniques to measure both cytosolic [Ca(+2)] and endoplasmic reticulum [Ca(+2)]. We found that the inhibitors of Bcl-2 protein interactions caused a slow and complete release of intracellular agonist-sensitive stores of calcium. The release was attenuated by inhibitors of IP(3)Rs and RyRs and substantially reduced by strong [Ca(2+)] buffering. Inhibition of IP(3)Rs and RyRs also dramatically reduced activation of apoptosis by BH3I-2'. CICR induced by different doses of BH3I-2' in Bcl-2 overexpressing cells was markedly decreased compared with control. The results suggest that Bcl-2 proteins regulate calcium release from the intracellular stores and suggest that the spatial-temporal patterns of agonist-stimulated cytosolic [Ca(+2)] changes are regulated by differential cellular distribution of interacting pairs of prosurvival and proapoptotic Bcl-2 proteins.

Publication types

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

MeSH terms

  • Animals
  • Apoptosis / drug effects
  • Benzamides / pharmacology
  • Benzopyrans / pharmacology
  • Calcium / metabolism*
  • Cell Line, Tumor
  • Endoplasmic Reticulum / metabolism
  • Inositol 1,4,5-Trisphosphate Receptors / antagonists & inhibitors
  • Inositol 1,4,5-Trisphosphate Receptors / physiology
  • Male
  • Mice
  • Nitriles / pharmacology
  • Pancreas, Exocrine / cytology
  • Pancreas, Exocrine / drug effects
  • Pancreas, Exocrine / metabolism*
  • Proto-Oncogene Proteins c-bcl-2 / antagonists & inhibitors*
  • Rats
  • Ryanodine Receptor Calcium Release Channel / drug effects
  • Ryanodine Receptor Calcium Release Channel / metabolism
  • bcl-2-Associated X Protein / metabolism
  • bcl-X Protein / antagonists & inhibitors

Substances

  • 3-iodo-5-chloro-N-(2-chloro-5-((4-chlorophenyl)sulphonyl)phenyl)-2-hydroxybenzamide
  • Bcl2l1 protein, mouse
  • Benzamides
  • Benzopyrans
  • Inositol 1,4,5-Trisphosphate Receptors
  • Nitriles
  • Proto-Oncogene Proteins c-bcl-2
  • Ryanodine Receptor Calcium Release Channel
  • bcl-2-Associated X Protein
  • bcl-X Protein
  • ethyl 2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate
  • Calcium