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

Resultado de la investigación: Article

64 Citas (Scopus)

Resumen

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.

Idioma originalEnglish
Páginas (desde-hasta)1026-1031
Número de páginas6
PublicaciónBiochemical and Biophysical Research Communications
Volumen159
N.º3
DOI
EstadoPublished - 31 mar 1989

Huella dactilar

Hypolipidemic Agents
Acyl Coenzyme A
Diglycerides
Coenzymes
Liver
Protein Kinase C
Rats
Nafenopin
Clofibric Acid
Bezafibrate
Peroxisome Proliferators
Phosphatidylserines
Phorbol Esters
Carcinogens
Tumors
Brain
Chemical activation
Enzymes
Pharmaceutical Preparations
Neoplasms

ASJC Scopus subject areas

  • Biochemistry
  • Biophysics
  • Molecular Biology

Citar esto

Bronfman, Miguel ; Orellana, Ariel ; Morales, M. Nelly ; Bieri, Francoise ; Waechter, Felix ; Stäubli, Willy ; Bentley, Philip. / Potentiation of diacylglycerol-activated protein kinase C by acyl-coenzyme a thioesters of hypolipidaemic drugs. En: Biochemical and Biophysical Research Communications. 1989 ; Vol. 159, N.º 3. pp. 1026-1031.
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Potentiation of diacylglycerol-activated protein kinase C by acyl-coenzyme a thioesters of hypolipidaemic drugs. / Bronfman, Miguel; Orellana, Ariel; Morales, M. Nelly; Bieri, Francoise; Waechter, Felix; Stäubli, Willy; Bentley, Philip.

En: Biochemical and Biophysical Research Communications, Vol. 159, N.º 3, 31.03.1989, p. 1026-1031.

Resultado de la investigación: Article

TY - JOUR

T1 - Potentiation of diacylglycerol-activated protein kinase C by acyl-coenzyme a thioesters of hypolipidaemic drugs

AU - Bronfman, Miguel

AU - Orellana, Ariel

AU - Morales, M. Nelly

AU - Bieri, Francoise

AU - Waechter, Felix

AU - Stäubli, Willy

AU - Bentley, Philip

PY - 1989/3/31

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AB - 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.

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