title: Novel phorbol analogs which bind to protein kinase C (PKC) without activation.
abstract: 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.
authors.affiliation: Faculty of Pharmaceutical Sciences, University of Tokyo, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Sugita
authors.forename: D
authors.initials: D
authors.lastname: Sawada
authors.forename: M
authors.initials: M
authors.lastname: Sodeoka
authors.forename: H
authors.initials: H
authors.lastname: Sasai
authors.forename: M
authors.initials: M
authors.lastname: Shibasaki
mesh_terms: 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*
chemical_list: D010703:Phorbol Esters; D015240:Phorbol 12,13-Dibutyrate; D011493:Protein Kinase C