Molecular mechanisms of muscarinic acetylcholine receptor-stimulated increase in cytosolic free Ca(2+) concentration and ERK1/2 activation in the MIN6 pancreatic β-cell line

Acta Diabetol. 2012 Aug;49(4):277-89. doi: 10.1007/s00592-011-0314-9. Epub 2011 Aug 11.

Abstract

Muscarinic acetylcholine receptor (mAChR) activation of pancreatic β-cells elevates intracellular Ca(2+) and potentiates glucose-stimulated insulin secretion. In addition, it activates a number of signaling molecules, including ERK1/2, whose activation has been shown to play an important role in regulating pancreatic β-cell function and mass. The aim of this work was to determine how mAChR activation elevates intracellular Ca(2+) concentration ([Ca(2+)]( i )) and activates ERK1/2 in the pancreatic β-cell line MIN6. We demonstrate that agonist-stimulated ERK1/2 activation is dependent on the activation of phospholipase C and an elevation in [Ca(2+)]( i ), but is independent of the activation of diacylglycerol-dependent protein kinase C isoenzymes. Using a pharmacological approach, we provide evidence that agonist-induced increases in [Ca(2+)]( i ) and ERK activity require (1) IP(3) receptor-mediated mobilization of Ca(2+) from the endoplasmic reticulum, (2) influx of extracellular Ca(2+) through store-operated channels, (3) closure of K(ATP) channels, and (4) Ca(2+) entry via L-type voltage-operated Ca(2+) channels. Moreover, this Ca(2+)-dependent activation of ERK is mediated via both Ras-dependent and Ras-independent mechanisms. In summary, this study provides important insights into the multifactorial signaling mechanisms linking mAChR activation to increases in [Ca(2+)]( i ) and ERK activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Calcium / metabolism*
  • Carbachol / pharmacology
  • Cell Line
  • Cholinergic Agonists / pharmacology
  • Enzyme Activation / physiology
  • Inositol 1,4,5-Trisphosphate Receptors / physiology
  • Insulin-Secreting Cells / metabolism*
  • Mitogen-Activated Protein Kinase 1 / metabolism*
  • Mitogen-Activated Protein Kinase 3 / metabolism
  • Phosphorylation
  • Receptors, Muscarinic / physiology*
  • Signal Transduction
  • Transfection
  • Type C Phospholipases / antagonists & inhibitors
  • Type C Phospholipases / metabolism

Substances

  • Cholinergic Agonists
  • Inositol 1,4,5-Trisphosphate Receptors
  • Receptors, Muscarinic
  • Carbachol
  • Mitogen-Activated Protein Kinase 1
  • Mitogen-Activated Protein Kinase 3
  • Type C Phospholipases
  • Calcium