title: Differential activation of protein kinase C isoforms by euxanthone, revealed by an in vivo yeast phenotypic assay.
abstract: The protein kinase C (PKC) modulatory effects of euxanthone, isolated from the wood of Cratoxylum maingayi, on isoforms alpha, betaI, delta, eta and zeta were characterised using an alternative in vivo yeast phenotypic assay. The present study shows that euxanthone can activate isoforms alpha, betaI, delta, eta and zeta, being more effective on PKC-betaI, -delta, -eta and -zeta than the established PKC activators used (the phorbol ester PMA and arachidonic acid for PKC-zeta). Furthermore, euxanthone presents differences on its potency towards individual PKC isoforms, showing a remarkable selectivity for PKC-zeta. These results can help to clarify the molecular basis of the euxanthone-mediated effects.
authors.forename: Lucília
authors.initials: L
authors.lastname: Saraiva
authors.forename: Paula
authors.initials: P
authors.lastname: Fresco
authors.forename: Eugénia
authors.initials: E
authors.lastname: Pinto
authors.forename: Anake
authors.initials: A
authors.lastname: Kijjoa
authors.forename: Maria José
authors.initials: MJ
authors.lastname: Gonzalez
authors.forename: Jorge
authors.initials: J
authors.lastname: Gonçalves
mesh_terms: D028084:Clusiaceae; D004305:Dose-Response Relationship, Drug; D006801:Humans; D020128:Inhibitory Concentration 50; D007527:Isoenzymes / Q000187:drug effects / Q000378:metabolism; D010641:Phenotype; D008517:Phytotherapy; D011493:Protein Kinase C / Q000187:drug effects* / Q000378:metabolism; D014966:Xanthenes / Q000008:administration & dosage / Q000494:pharmacology*; D044004:Xanthones; D015003:Yeasts / Q000187:drug effects* / Q000235:genetics / Q000378:metabolism
chemical_list: D007527:Isoenzymes; D014966:Xanthenes; D044004:Xanthones; C404221:euxanthone; D011493:Protein Kinase C