title: [Comparative investigation of the effect of calix[4]arene C-99 and its analogs on Na+,K(+)-ATPase activity of uterus myocite plasma membrane].
abstract: The aim of our investigation was to determine structural features of calix[4]arene C-99 which are important for its inhibition properties relative to Na+,K(+)-ATPase of uterus myocite plasma membrane. Therefore we studied the effect of calix[4]arenes C-296, C-297, C-424, C-425, C-426, C-427, which are structurally similar to this inhibitor, on the mentioned enzyme activity. We have shown that calixarenes C-296 and C-297 which have two additional propoxy groups on the lower rim of macrocycle are less effective inhibitors of Na+,K(+)-ATPase relative to calixarene C-99. Calixarenes C-425 and C-427 which have on the upper rim of macrocycle three and four phosponic residues, respectively, also inhibit Na+,K(+)-ATPase activity less effectively as compared to calixarene C-99. Both calixarenes: C-424, which has only two carbonate residues on the upper rim, and C-426, which has on the upper rim ketomethilphosphonate residues instead of hydroxymethilphosphonate residues of calixarene C-99, do not affect Na+,K(+)-ATPase activity. We have made respective conclusions concerning the role of certain chemical groups of calixarene C-99 during its interaction with Na+,K(+)-ATPase.
authors: T O
authors: TO
authors: Veklich
authors: O A
authors: OA
authors: Shkrabak
authors: S O
authors: SO
authors: Cherenok
authors: V I
authors: VI
authors: Kal'chenko
authors: S O
authors: SO
authors: Kosterin
mesh_terms: D000818:Animals; D017301:Ca(2+) Mg(2+)-ATPase / Q000378:metabolism; D047250:Calixarenes / Q000138:chemical synthesis / Q000494:pharmacology*; D002462:Cell Membrane / Q000187:drug effects* / Q000201:enzymology; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000494:pharmacology; D005260:Female; D007700:Kinetics; D032389:Myocytes, Smooth Muscle / Q000166:cytology / Q000187:drug effects* / Q000201:enzymology; D009215:Myometrium / Q000166:cytology / Q000187:drug effects / Q000201:enzymology; D010042:Ouabain / Q000494:pharmacology; D000254:Sodium-Potassium-Exchanging ATPase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013552:Swine
chemical_list: D004791:Enzyme Inhibitors; D047250:Calixarenes; D010042:Ouabain; D017301:Ca(2+) Mg(2+)-ATPase; D000254:Sodium-Potassium-Exchanging ATPase