Molecular mechanism of calcium channel regulation in the fight-or-flight response

Sci Signal. 2010 Sep 28;3(141):ra70. doi: 10.1126/scisignal.2001152.

Abstract

During the fight-or-flight response, the sympathetic nervous system stimulates L-type calcium ion (Ca2+) currents conducted by Ca(V)1 channels through activation of β-adrenergic receptors, adenylyl cyclase, and phosphorylation by adenosine 3',5'-monophosphate-dependent protein kinase [also known as protein kinase A (PKA)], increasing contractility of skeletal and cardiac muscles. We reconstituted this regulation of cardiac Ca(V)1.2 channels in non-muscle cells by forming an autoinhibitory signaling complex composed of Ca(V)1.2Δ1800 (a form of the channel truncated at the in vivo site of proteolytic processing), its noncovalently associated distal carboxyl-terminal domain, the auxiliary α₂δ₁ and β(2b) subunits, and A-kinase anchoring protein 15 (AKAP15). A factor of 3.6 range of Ca(V)1.2 channel activity was observed from a minimum in the presence of protein kinase inhibitors to a maximum upon activation of adenylyl cyclase. Basal Ca(V)1.2 channel activity in unstimulated cells was regulated by phosphorylation of serine-1700 and threonine-1704, two residues located at the interface between the distal and the proximal carboxyl-terminal regulatory domains, whereas further stimulation of channel activity through the PKA signaling pathway only required phosphorylation of serine-1700. Our results define a conceptual framework for Ca(V)1.2 channel regulation and identify sites of phosphorylation that regulate channel activity.

Publication types

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

MeSH terms

  • A Kinase Anchor Proteins / physiology
  • Amino Acid Sequence
  • Animals
  • Calcium Channels, L-Type / chemistry
  • Calcium Channels, L-Type / physiology*
  • Cyclic AMP-Dependent Protein Kinases / metabolism
  • Fear*
  • Membrane Proteins / physiology
  • Models, Molecular
  • Phosphorylation
  • Signal Transduction
  • Stress, Psychological*

Substances

  • A Kinase Anchor Proteins
  • AKAP7 protein, human
  • Calcium Channels, L-Type
  • L-type calcium channel alpha(1C)
  • Membrane Proteins
  • Cyclic AMP-Dependent Protein Kinases