title: [Effect of N-3-methyladenine on peptidase and ribonuclease activity of proteasome].
abstract: Using a culture of cardiomyocytes it has been shown, that a well-known inhibitor of autophagy, N-3-methyladenine causes a 1.4 fold increase (p = 0.023) of the chymotrypsin-like activity, a 1.5 fold increase (p = 0.09) of the peptidyl-glutamyl peptide-hydrolyzing activity and 1.5 fold decrease (p = 0.07) of the trypsin-like activity of the proteasome. N-3-methyladenine in a dose-dependent manner inhibits chymotrypsin-like and peptidyl-glutamyl peptide-hydrolyzing activities of the purified 20S proteasome, but activates it trypsin-like activity. Chymotrypsin-like and peptidyl-glutamyl peptide-hydrolyzing activities of the 26S proteasome from proteasome fraction II did change in the same way, as in the case of 20S proteasome, but trypsin-like activity decreased. Using the above method of determining ribonuclease activity, we have shown, that N-3-methyladenine and clasto-lactacystin b-lactone inhibit the RNase activity of the proteasome. Specific proteasome inhibitor exhibits more powerful action, almost completely preventing RNA of actin and myosin from degradation. These data show a multitarget action of N-3-methyladenine, resulting in changes of peptidase and ribonuclease activity of the proteasome.
authors.forename: V E
authors.initials: VE
authors.lastname: Dosenko
authors.forename: V Iu
authors.initials: VIu
authors.lastname: Zagoriĭ
authors.forename: V S
authors.initials: VS
authors.lastname: Nagibin
authors.forename: A A
authors.initials: AA
authors.lastname: Moĭbenko
mesh_terms: D000225:Adenine / Q000031:analogs & derivatives* / Q000494:pharmacology; D000818:Animals; D000831:Animals, Newborn; D001343:Autophagy / Q000187:drug effects*; D002478:Cells, Cultured; D004305:Dose-Response Relationship, Drug; D051379:Mice; D032383:Myocytes, Cardiac / Q000187:drug effects / Q000201:enzymology; D010447:Peptide Hydrolases / Q000378:metabolism; D011480:Protease Inhibitors / Q000494:pharmacology*; D046988:Proteasome Endopeptidase Complex / Q000378:metabolism*; D061988:Proteasome Inhibitors; D011817:Rabbits; D051381:Rats; D012260:Ribonucleases / Q000037:antagonists & inhibitors / Q000378:metabolism*
chemical_list: D011480:Protease Inhibitors; D061988:Proteasome Inhibitors; C025946:3-methyladenine; D012260:Ribonucleases; D010447:Peptide Hydrolases; D046988:Proteasome Endopeptidase Complex; D000225:Adenine