Kinetic evidence that 1,2-diolein inhibits phorbol ester binding to protein kinase C via a competitive mechanism |
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Authors: | N A Sharkey P M Blumberg |
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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. |
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