Phorbol ester effects on alpha 1-adrenoceptor binding and phosphatidylinositol metabolism in cultured vascular smooth muscle cells.

Published

Journal Article

Tumor promoting phorbol esters stimulate Ca++ phospholipid-dependent protein kinase C. It has been suggested that this enzyme regulates the functional properties of different cell membrane receptors. In this study we investigated the effect of phorbol esters on alpha 1-adrenoceptor binding and phosphatidylinositol metabolism in cultured smooth muscle cells derived from rabbit aorta. Treatment of these cells with biologically active phorbol esters for 15 min. to 2 hours caused a marked decrease of norepinephrine stimulation of inositol phospholipid metabolism and a 3 fold decrease in agonist affinity for 125I-HEAT binding to alpha 1-adrenoceptors in the intact smooth muscle cells. The ability of phorbol esters to modulate alpha 1-adrenoceptor responsiveness suggests that activation of protein kinase C may represent an important mechanism regulating alpha 1-adrenergic receptor functional properties.

Full Text

Duke Authors

Cited Authors

  • Cotecchia, S; Leeb-Lundberg, LM; Hagen, PO; Lefkowitz, RJ; Caron, MG

Published Date

  • December 23, 1985

Published In

Volume / Issue

  • 37 / 25

Start / End Page

  • 2389 - 2398

PubMed ID

  • 3001461

Pubmed Central ID

  • 3001461

International Standard Serial Number (ISSN)

  • 0024-3205

Digital Object Identifier (DOI)

  • 10.1016/0024-3205(85)90106-7

Language

  • eng

Conference Location

  • Netherlands