Kinetic evidence that 1,2-diolein inhibits phorbol ester binding to protein kinase C via a competitive mechanism.

Abstract:

:Diacylglycerols inhibit binding of [20-3H]phorbol 12,13-dibutyrate ([3H]PDBu) to protein kinase C (the phorbol ester receptor). This inhibition could reflect competitive binding by the diglyceride. Alternatively, it might simply represent perturbation of the lipid environment required for binding activity. As predicted for a competitive mechanism, we report here that inhibitory concentrations of the diglyceride 1,2-diolein do not affect the off-rate of [3H]PDBu from its receptor. This behavior contrasts with that of arachidonic acid, which appears to interact via a mixed mechanism.

authors

Sharkey NA,Blumberg PM

doi

10.1016/0006-291x(85)91242-2

subject

Has Abstract

pub_date

1985-12-31 00:00:00

pages

1051-6

issue

3

eissn

0006-291X

issn

1090-2104

pii

0006-291X(85)91242-2

journal_volume

133

pub_type

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