The inhibition of rat liver chromatin protease by congeners of the phenylboronic acids.
A group of arylalkylboronic acids were synthesized in order to investigate the inhibitory potential of these compounds for rat liver chromatin protease (EC 3.4--). The effect of side chain length, side chain substitution and aromatic substitution on proteolytic activity in chromatin dissociated in salt and urea was assayed. It was determined that a side chain length two carbons long provided the greatest inhibitory effect with complete inhibition attainable at 20 mM concentration of phenylethylboronic acid. Aryl substitution in the ortho position proved to be the most potent structural change with complete inhibition attained by 1 mM concentration of 0-methylphenylethylboronic acid. The binding of these two inhibitors proved to be reversible.
D000818:Animals; D001897:Boronic Acids / Q000494:pharmacology*; D002843:Chromatin; D004305:Dose-Response Relationship, Drug; D008099:Liver / Q000201:enzymology*; D010447:Peptide Hydrolases; D011480:Protease Inhibitors; D011485:Protein Binding; D051381:Rats; D013329:Structure-Activity Relationship
D001897:Boronic Acids; D002843:Chromatin; D011480:Protease Inhibitors; D010447:Peptide Hydrolases; C019896:chromatin protease