[The inhibitory effect of a third generation retinoid, R8605, on protein kinase C activity in vitro].
R8605 is a newly synthesized compound of the third generation retinoids produced by the Institute of Materia Medica. It exhibited in vitro inhibitory effects on the diolein and TPA (12-O-tetradecanoylphorbol-13-acetate) induced activation of Protein Kinase C (PKC) from rat brain and also showed inhibitory effects on the calcium/phospholipid-independent phosphorylation of protamine by PKC. The IC50 values were 65, 70, 100/mumol/L respectively. It is suggested that the inhibition of PKC activity by R8605 is related to the inhibition of tumor promotion.
Sun
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Institute of Materia Medica, Beijing.
D000818:Animals; D004075:Diglycerides / Q000037:antagonists & inhibitors; D005260:Female; D008297:Male; D010766:Phosphorylation / Q000187:drug effects; D011479:Protamines / Q000378:metabolism; D011493:Protein Kinase C / Q000037:antagonists & inhibitors / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains; D012176:Retinoids / Q000494:pharmacology*; D013755:Tetradecanoylphorbol Acetate / Q000737:chemistry
D004075:Diglycerides; D011479:Protamines; D012176:Retinoids; C073874:R 8605; D011493:Protein Kinase C; D013755:Tetradecanoylphorbol Acetate; C013965:diolein