Diacylglycerol modulates binding and phosphorylation of the epidermal growth factor receptor.

摘要: Tumor promoters cause a variety of effects in cultured cells, at least some which are thought to result from activation the Ca2+-phospholipid-stimulated protein kinase C. One action tumor is modulation binding and phosphorylation epidermal growth factor (EGF) receptor A431 cells. To determine if these compounds act on EGF by substituting for endogenous activator C kinase, diacylglycerol, we compared potent promoter 12-O-tetradecanoyl phorbol 13-acetate (TPA) with those synthetic diacylglycerol analog 1-oleyl 2-acetyl diglycerol (OADG). When cells were treated TPA, subcellular distribution activity shifted predominantly cytosolic location membrane-associated state; OADG also caused disappearance activity. The shift TPA or OADG, correlated changes receptor. like loss an apparent high affinity class receptors, blocked EGF-induced tyrosine receptor, stimulated both serine threonine residues. No difference between phosphopeptide maps receptors was observed. Thus, it appears that can exert their presumably activating Further, results suggest endogenously produced may have role normal regulatory pathways.