Ca2+ influx through L-type Ca2+ channels and Ca2+-induced Ca2+ release regulate cAMP accumulation and Epac1-dependent ERK 1/2 activation in INS-1 cells

Mol Cell Endocrinol. 2016 Jan 5:419:60-71. doi: 10.1016/j.mce.2015.09.034. Epub 2015 Oct 3.

Abstract

We previously reported that INS-1 cells expressing the intracellular II-III loop of the L-type Ca(2+) channel Cav1.2 (Cav1.2/II-III cells) are deficient in Ca(2+)-induced Ca(2+) release (CICR). Here we show that glucose-stimulated ERK 1/2 phosphorylation (GSEP) is slowed and reduced in Cav1.2/II-III cells compared to INS-1 cells. This parallels a decrease in glucose-stimulated cAMP accumulation (GS-cAMP) in Cav1.2/II-III cells. Influx of Ca(2+) via L-type Ca(2+) channels and CICR play roles in both GSEP and GS-cAMP in INS-1 cells since both are inhibited by nicardipine or ryanodine. Further, the Epac1-selective inhibitor CE3F4 abolishes glucose-stimulated ERK activation in INS-1 cells, as measured using the FRET-based sensor EKAR. The non-selective Epac antagonist ESI-09 but not the Epac2-selective antagonist ESI-05 nor the PKA antagonist Rp-cAMPs inhibits GSEP in both INS-1 and Cav1.2/II-III cells. We conclude that L-type Ca(2+) channel-dependent cAMP accumulation, that's amplified by CICR, activates Epac1 and drives GSEP in INS-1 cells.

Keywords: Ca(2+)-induced Ca(2+) release; Ca(v)1.2; Exchange protein directly activated by cAMP; Extracellular signal regulated kinase 1/2; L-type Ca(2+) channel; Pancreatic beta-cell; cAMP.

Publication types

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

MeSH terms

  • Animals
  • Benzene Derivatives / pharmacology
  • Calcium / metabolism*
  • Calcium Channels, L-Type / metabolism*
  • Cyclic AMP / metabolism*
  • Glucose / pharmacology
  • Guanine Nucleotide Exchange Factors / metabolism*
  • MAP Kinase Signaling System* / drug effects
  • Nicardipine / pharmacology
  • Phosphorylation / drug effects
  • Quinolines / pharmacology
  • Rats
  • Ryanodine / pharmacology
  • Sulfones / pharmacology

Substances

  • 6-fluoro-5,7-dibromo-2-methyl-1-formyl-1,2,3,4-tetrahydroquinoline
  • Benzene Derivatives
  • Calcium Channels, L-Type
  • ESI-05
  • Guanine Nucleotide Exchange Factors
  • Quinolines
  • Rapgef3 protein, rat
  • Sulfones
  • Ryanodine
  • Nicardipine
  • Cyclic AMP
  • Glucose
  • Calcium