Phosphorylation of the purified receptor for calcium channel blockers by cAMP kinase and protein kinase C

Eur J Biochem. 1987 Nov 16;169(1):137-42. doi: 10.1111/j.1432-1033.1987.tb13590.x.

Abstract

The dihydropyridine receptor purified from rabbit skeletal muscle contains three proteins of 165, 55 and 32 kDa. cAMP kinase and protein kinase C phosphorylate the 165-kDa and the 55-kDa proteins. At identical concentrations of each protein kinase, cAMP kinase phosphorylates the 165-kDa protein faster than the 55-kDa protein. Protein kinase C phosphorylates preferentially the 55-kDa protein. cAMP kinase incorporates up to 1.6 mol phosphate/mol protein into the 165-kDa protein and 1 mol/mol into the 55-kDa protein upon prolonged incubation. At a physiological concentration of cAMP kinase 1 mol phosphate is incorporated/mol 165-kDa protein within 10 min, suggesting a physiological role of this phosphorylation. Protein kinase C incorporates up to 1 mol phosphate/mol into the 55-kDa protein and less than 1 mol/mol into the 165-kDa protein. Tryptic phosphopeptide analysis reveals that cAMP kinase phosphorylates two distinct peptides in the 165-kDa protein, whereas protein kinase C phosphorylates a single peptide in the 165-kDa protein. cAMP kinase and protein kinase C phosphorylate three and two peptides in the 55-kDa protein, respectively. Mixtures of the tryptic phosphopeptides derived from the 165-kDa and 55-kDa proteins elute according to the composite of the two elution profiles. These results suggest that the 165-kDa protein, which contains the binding sites for each class of calcium channel blockers and the basic calcium-conducting structure, is a specific substrate for cAMP kinase. The 55-kDa protein apparently contains sites preferentially phosphorylated by protein kinase C.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Calcium Channels
  • Cattle
  • Chromatography, Gel
  • Chromatography, High Pressure Liquid
  • Cyclic AMP / pharmacology*
  • Kinetics
  • Microsomes / analysis
  • Muscles / analysis
  • Peptide Fragments / metabolism
  • Phosphorylation
  • Protein Kinase C / metabolism*
  • Protein Kinases / metabolism*
  • Rabbits
  • Rats
  • Receptors, Nicotinic / metabolism*
  • Substrate Specificity
  • Trypsin / metabolism

Substances

  • Calcium Channels
  • Peptide Fragments
  • Receptors, Nicotinic
  • Cyclic AMP
  • Protein Kinases
  • Protein Kinase C
  • Trypsin