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

Abstract

Modulation of ion channels is an essential step for understanding the regulation of cellular functions. 1,4-Dihydropyridines (nitrendipine, 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.

• Authors: J Navarro
• Journal: The Journal of biological chemistry (J Biol Chem) Vol. 262 Issue 10 Pg. 4649-52 (Apr 05 1987) ISSN: 0021-9258 [Print] United States
• PMID: 2435714 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, Non-P.H.S.)

Chemical References

• Calcium Channel Blockers
• Calcium Channels
• Diglycerides
• Ion Channels
• Receptors, Nicotinic
• 1-oleoyl-2-acetylglycerol
• Protein Kinase C
• Tetradecanoylphorbol Acetate
• Calcium

Topics

• Animals
• Calcium (metabolism)
• Calcium Channel Blockers (metabolism, pharmacology)
• Calcium Channels
• Cells, Cultured
• Chick Embryo
• Diglycerides (pharmacology)
• Enzyme Activation (drug effects)
• Ion Channels (drug effects, metabolism)
• Muscles (metabolism)
• Protein Kinase C (metabolism)
• Receptors, Nicotinic (drug effects, metabolism)
• Tetradecanoylphorbol Acetate (pharmacology)