Phenobarbital competes with diacylglycerol for protein kinase C.
Phenobarbital inhibits protein kinase C of rat brain by competitively displacing the effector of the enzyme, diacylglycerol. The drug appears to occupy the triple hydrogen bonding site which bonds diacylglycerol - and also phorbol esters - to the enzyme. It remains to be seen if the effect is responsible for the pharmaceutical activity of the drug; even so, it provides an example of a restructuring of lipid-protein hydrogen bonding, in the hydrogen belt of the membrane, in a manner postulated as a mechanism of anesthesia.
D001665:Binding Sites; D001667:Binding, Competitive; D004075:Diglycerides / Q000378:metabolism / Q000494:pharmacology*; D004789:Enzyme Activation / Q000187:drug effects; D005989:Glycerides / Q000494:pharmacology*; D008958:Models, Molecular; D010634:Phenobarbital / Q000378:metabolism / Q000494:pharmacology*; D011493:Protein Kinase C / Q000037:antagonists & inhibitors / Q000378:metabolism*
C011439:1,2-diacylglycerol; D004075:Diglycerides; D005989:Glycerides; D011493:Protein Kinase C; D010634:Phenobarbital