Inhibition of protein kinase C by semisynthetic phospholipid plasmanyl-(N-acyl)-ethanolamine, a nontoxic antitumor preparation.
Protein kinase C was extracted from mouse brain and partially purified by ion-exchange chromatography on a DEAE-cellulose column. Its activity was determined by incorporation of phosphate from [gamma-32P]ATP into histone H2b. The semisynthetic alkyl-phospholipid plasmanyl-(N-acyl)-ethanolamine (PNAEs) with selective antitumor activity inhibited the activity of the protein kinase in a cell-free system in the presence of phosphatidylserine, a protein kinase C activator. The inhibition was competitive with respect to phosphatidylserine, the inhibition constant being 40 microM.
Mikhaevich
I S
IS
Research Institute of Experimental Diagnosis and Therapy of Tumors, Academy of Medical Sciences, Moscow.
Gerasimova
G K
GK
Kára
J
J
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology; D001665:Binding Sites; D001921:Brain / Q000201:enzymology; D002457:Cell Extracts; D002848:Chromatography, DEAE-Cellulose; D005260:Female; D007700:Kinetics; D051379:Mice; D008809:Mice, Inbred C3H; D010718:Phosphatidylserines / Q000494:pharmacology*; D010742:Phospholipid Ethers / Q000378:metabolism / Q000494:pharmacology*; D011493:Protein Kinase C / Q000037:antagonists & inhibitors* / Q000302:isolation & purification / Q000378:metabolism
D000970:Antineoplastic Agents; D002457:Cell Extracts; D010718:Phosphatidylserines; D010742:Phospholipid Ethers; D011493:Protein Kinase C