(-)-Indolactam V activates protein kinase C and induces changes in muscarinic receptor functions in SH-SY5Y human neuroblastoma cells.

Abstract

The effects of a synthetic protein kinase C (PKC) activator, (-)-indolactam V (ILV), were studied in SH-SY5Y human neuroblastoma cells. (-)-ILV induced a translocation of PKC from cytosol to plasma membrane and displaced 3H-phorbol dibutyrate binding in the micromolar range. In addition, (-)-ILV caused a decreased sensitivity of cells to muscarinic agonist-induced Ca2+ mobilization measured with quin-2 and induced a down-regulation of cell surface muscarinic receptors. All the changes induced by (-)-ILV were similar in magnitude to those seen with the phorbol ester tetradecanoyl phorbol acetate (TPA). The results suggest that (-)-ILV is a full activator of PKC and a promising alternative to phorbol esters in studies on mechanism of actions of PKC.

• Authors: J Heikkilä, K E Akerman
• Journal: Biochemical and biophysical research communications (Biochem Biophys Res Commun) Vol. 162 Issue 3 Pg. 1207-13 (Aug 15 1989) ISSN: 0006-291X [Print] United States
• PMID: 2764930 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Indoles
• Lactams
• Receptors, Muscarinic
• Phorbol 12,13-Dibutyrate
• indolactam V
• Protein Kinase C
• Tetradecanoylphorbol Acetate
• Calcium

Topics

• Calcium (physiology)
• Cell Compartmentation (drug effects)
• Cell Differentiation (drug effects)
• Cell Membrane (enzymology)
• Enzyme Activation (drug effects)
• Humans
• Indoles (pharmacology)
• Lactams (pharmacology)
• Neuroblastoma (enzymology, pathology)
• Phorbol 12,13-Dibutyrate (metabolism)
• Protein Kinase C (metabolism)
• Receptors, Muscarinic (physiology)
• Tetradecanoylphorbol Acetate (pharmacology)
• Tumor Cells, Cultured