Potentiation of diacylglycerol-activated protein kinase C by acyl-coenzyme a thioesters of hypolipidaemic drugs

Miguel Bronfman, Ariel Orellana, M. Nelly Morales, Francoise Bieri, Felix Waechter, Willy Stäubli, Philip Bentley

Research output: Contribution to journalArticlepeer-review

65 Citations (Scopus)

Abstract

Acyl-Coenzyme A thioesters of the hypolipidaemic and cancerinogenic peroxisome proliferators clofibric acid, nafenopin, ciprofibrate, bezafibrate and tibric acid were found to greatly increase the activity of rat brain protein kinase C. Maximal activation required the simultaneous presence of Ca+2, phosphatidylserine and diolein, thus differentiating their action from that of other tumor promoters such as phorbol esters. Under similar conditions the unesterified drugs were comparatively ineffective. Similar results were obtained using the rat liver enzyme. The data suggest that acyl-coenzyme A thioesters of hypolipidaemic drugs, may play a role in the induction of liver tumors by these compounds, through the potentiation of protein kinase C.

Original languageEnglish
Pages (from-to)1026-1031
Number of pages6
JournalBiochemical and Biophysical Research Communications
Volume159
Issue number3
DOIs
Publication statusPublished - 31 Mar 1989

ASJC Scopus subject areas

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology

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