Modulation of [3H]dihydropyridine receptors by activation of protein kinase C in chick muscle cells

Research output: Contribution to journalArticle

26 Scopus citations

Abstract

Modulation of ion channels is an essential step for understanding the regulation of cellular functions. 1,4-Dihydropyridines (nitrendepine, nifedipine, PN 200-110, etc.) are potent inhibitors of voltage-dependent calcium channels and are important therapeutic agents in the treatment of various cardiovascular disorders such as angina and cardiac arrhythmias. In this work a new procedure is employed to determine the density of surface dihydropyridine receptors in contracting muscle cells in culture. Activation of endogenous protein kinase C (the Ca2+/phospholipid-dependent enzyme) by the tumor promoter phorbol-12-myristate or 1-oleoyl-2-acetylglycerol enhanced the number of dihydropyridine receptors without significant change in the receptor affinity. The increase in the number of receptors was associated with stimulation of the dihydropyridine-sensitive 45Ca uptake as well as activation of protein kinase C in myotubes treated with phorbol esters. These data strongly suggest that activation of protein kinase C promotes the appearance of dihydropyridine receptors in the plasma membrane.

Original languageEnglish (US)
Pages (from-to)4649-4652
Number of pages4
JournalJournal of Biological Chemistry
Volume262
Issue number10
StatePublished - Jan 1 1987
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Cell Biology

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