title: [Inhibitory action of polycationic peptides on hormonal regulation of adenylyl cyclase of the ciliate Dileptus anser].
abstract: To analyse molecular mechanisms of regulatory action of different hormones on the activity of the adenylyl cyclase signaling system (ACS) of the ciliate Dileptus anser, we studied the influence on this process of six synthetic polycationic peptides and peptides, corresponding to C-terminal regions of mammalian G-protein 385-394 alphas- and 346-355 alphai2-subunits. As we reported earlier, these peptides block hormonal signal transduction in tissues of the higher eukaryotes. Now it has been found that both polycationic peptides, containing hydrophobic C to-radicals, and branched peptides decrease regulatory effects of peptide hormones (insulin, relaxin) and biogenic amines (serotonin, adrenaline) on adenylyl cyclase (AC) activity and GTP-binding. In regard to the following peptides Cys-epsilonAhx-Trp-Lys-Lys(C10)-Lys2-Lys(C10)-Lys3-Lys(C10)-Tyr-Lys-Lys(C10)-Lys-Lys-amide and [(Gly-Arg-Gly-Asp-Ser-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Pro- Pro-Gly)2-Lys-EAhx-Cys]2 (epsilonAhx - E-aminocaproyl, C10 - caprinoyl group) their dose-dependent inhibitory action is shown. In cell culture of D. anser with a lower basal AC activity, both hydrophobic and branched peptides stimulated AC and GTP-binding without hormones. The data give evidence that these peptides can activate ACS of ciliates in a receptor-independent manner. No influence of peptides 385-394 alphas and 346-355 alphai2 on hormonal signal transduction in D. anser was observed, due, presumably, to some structural differences of G-proteins of the lower and higher eukaryotes. A conclusion was made about an important role of polycationic regions for functional coupling of hormone-activated receptor and G-proteins in the ciliate D. anser.
authors.forename: A O
authors.initials: AO
authors.lastname: Shpakov
authors.forename: K V
authors.initials: KV
authors.lastname: Derkach
authors.forename: I A
authors.initials: IA
authors.lastname: Gur'ianov
authors.forename: Z I
authors.initials: ZI
authors.lastname: Uspenskaia
authors.forename: L A
authors.initials: LA
authors.lastname: Kuznetsova
authors.forename: S A
authors.initials: SA
authors.lastname: Plesneva
authors.forename: G P
authors.initials: GP
authors.lastname: Vlasov
authors.forename: M N
authors.initials: MN
authors.lastname: Pertseva
mesh_terms: D000262:Adenylyl Cyclases / Q000378:metabolism*; D000818:Animals; D001679:Biogenic Amines / Q000494:pharmacology; D016798:Ciliophora / Q000187:drug effects / Q000201:enzymology*; D004305:Dose-Response Relationship, Drug; D004789:Enzyme Activation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D036361:Peptide Hormones / Q000494:pharmacology; D010455:Peptides / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D001679:Biogenic Amines; D004791:Enzyme Inhibitors; D036361:Peptide Hormones; D010455:Peptides; D000262:Adenylyl Cyclases