Novel phorbol analogs which bind to protein kinase C (PKC) without activation.
13-Deacetoxy-11-demethyl-phorbol derivatives with acyl groups of various lengths (from hexanoyl to tetradecanoyl) at the C-12 position were synthesized in an optically active form. Although considerable binding affinities to PKC were observed by analogs 3-7, no activation of PKC was seen even at 10 microM.
Sugita
K
K
Faculty of Pharmaceutical Sciences, University of Tokyo, Japan.
Sawada
D
D
Sodeoka
M
M
Sasai
H
H
Shibasaki
M
M
D001667:Binding, Competitive / Q000187:drug effects; D004789:Enzyme Activation / Q000187:drug effects; D015240:Phorbol 12,13-Dibutyrate / Q000378:metabolism; D010703:Phorbol Esters / Q000138:chemical synthesis / Q000378:metabolism*; D011485:Protein Binding; D011493:Protein Kinase C / Q000378:metabolism*
D010703:Phorbol Esters; D015240:Phorbol 12,13-Dibutyrate; D011493:Protein Kinase C