Protein kinase C isoforms differentially phosphorylate Ca(v)1.2 alpha(1c)

Biochemistry. 2009 Jul 21;48(28):6674-83. doi: 10.1021/bi900322a.

Abstract

The regulation of Ca(2+) influx through the phosphorylation of the L-type Ca(2+) channel, Ca(v)1.2, is important for the modulation of excitation-contraction (E-C) coupling in the heart. Ca(v)1.2 is thought to be the target of multiple kinases that mediate the signals of both the renin-angiotensin and sympathetic nervous systems. Detailed biochemical information regarding the protein phosphorylation reactions involved in the regulation of Ca(v)1.2 is limited. The protein kinase C (PKC) family of kinases can modulate cardiac contractility in a complex manner, such that contractility is either enhanced or depressed and relaxation is either accelerated or slowed. We have previously reported that Ser(1928) in the C-terminus of alpha(1c) was a target for PKCalpha, -zeta, and -epsilon phosphorylation. Here, we report the identification of seven PKC phosphorylation sites within the alpha(1c) subunit. Using phospho-epitope specific antibodies to Ser(1674) and Ser(1928), we demonstrate that both sites within the C-terminus are phosphorylated in HEK cells in response to PMA. Phosphorylation was inhibited with a PKC inhibitor, bisindolylmaleimide. In Langendorff-perfused rat hearts, both Ser(1674) and Ser(1928) were phosphorylated in response to PMA. Phosphorylation of Ser(1674), but not Ser(1928), is PKC isoform specific, as only PKCalpha, -betaI, -betaII, -gamma, -delta, and -theta, but not PKCepsilon, -zeta, and -eta, were able to phosphorylate this site. Our results identify a molecular mechanism by which PKC isoforms can have different effects on channel activity by phosphorylating different residues.

Publication types

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

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Calcium Channels, L-Type / metabolism*
  • Cell Line
  • Humans
  • In Vitro Techniques
  • Isoenzymes / chemistry
  • Isoenzymes / metabolism
  • Mice
  • Mice, Knockout
  • Molecular Sequence Data
  • Myocytes, Cardiac / drug effects
  • Myocytes, Cardiac / enzymology
  • Phosphorylation / drug effects
  • Phosphoserine / metabolism
  • Protein Kinase C / chemistry
  • Protein Kinase C / metabolism*
  • Protein Structure, Secondary
  • Rabbits
  • Rats
  • Recombinant Fusion Proteins / metabolism
  • Tetradecanoylphorbol Acetate / pharmacology

Substances

  • Calcium Channels, L-Type
  • Isoenzymes
  • L-type calcium channel alpha(1C)
  • Recombinant Fusion Proteins
  • Phosphoserine
  • Protein Kinase C
  • Tetradecanoylphorbol Acetate