title: Inhibition in vitro of yeast DNA polymerase I activity by beta-blockers.
abstract: The activity of DNA polymerase I from Saccharomyces cerevisiae is inhibited, in a dose-dependent fashion, by the oncogenic beta-blocker 1-(2-nitro-3-methyl-phenoxy)-3-tert-butylamino-propan-2-ol (ZAMI 1305) and by the non-oncogenic beta-blockers 1-(2-nitro-5-methyl-phenoxy)-3-tert-butylamino-propan-2-ol (ZAMI 1327), atenolol, and propranolol, the latter having the highest inhibiting activity. The inhibition is due to an interaction of the beta-blockers with the free enzyme and with the enzyme-DNA complex. The degree of inhibition is directly related to the hydrophobicity of the aromatic moiety and to the length and hydrophilicity of the aliphatic chain of the inhibitor. No relation seems to exist between the in vitro inhibition of yeast DNA polymerase I by beta-blockers and their oncogenic activity.
mesh_terms: D000319:Adrenergic beta-Antagonists / Q000494:pharmacology*; D001262:Atenolol / Q000494:pharmacology; D002273:Carcinogens / Q000494:pharmacology; D002474:Cell-Free System; D004256:DNA Polymerase I / Q000037:antagonists & inhibitors*; D019384:Nucleic Acid Synthesis Inhibitors; D011412:Propanolamines / Q000494:pharmacology*; D011433:Propranolol / Q000494:pharmacology; D012441:Saccharomyces cerevisiae / Q000201:enzymology*; D013329:Structure-Activity Relationship
chemical_list: D000319:Adrenergic beta-Antagonists; D002273:Carcinogens; D019384:Nucleic Acid Synthesis Inhibitors; D011412:Propanolamines; D001262:Atenolol; C028476:Zami 1327; C028475:ZAMI 1305; D011433:Propranolol; D004256:DNA Polymerase I