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.

[1]  P. C. Huang,et al.  Effect of protein-bound RNA associated with chick embryo chromatin on template specificity of the chromatin. , 1969, Journal of molecular biology.

[2]  D. Carter,et al.  Degradation of chromosomal proteins during dissociation and reconstitution of chromatin. , 1974, Biochemical and biophysical research communications.

[3]  J. Garrels,et al.  A histone protease of rat liver chromatin. , 1972, Biochemical and biophysical research communications.

[4]  M. Furlan,et al.  Protein catabolism in thymus nuclei. II. Binding of histone-splitting nuclear proteases to deoxyribonucleic acid. , 1967, Biochimica et biophysica acta.

[5]  P. Ganguly.  Isolation and properties of a thrombin-sensitive protein from human blood platelets. , 1971, The Journal of biological chemistry.

[6]  G. Lienhard,et al.  The binding of boronic acids to chymotrypsin. , 1974, Biochemistry.

[7]  Carter Db,et al.  Chromatin-bound protease: degradation of chromosomal proteins under chromatin dissociation conditions. , 1976 .

[8]  U. K. Laemmli,et al.  Cleavage of Structural Proteins during the Assembly of the Head of Bacteriophage T4 , 1970, Nature.

[9]  G. E. Branch,et al.  The Relative Strengths of Some Hydrocarbon Derivatives of Boric Acid , 1934 .

[10]  G. Lienhard,et al.  2-phenylethaneboronic acid, a possible transition-state analog for chymotrypsin. , 1971, Biochemistry.

[11]  Frederick R. Bean,et al.  DERIVATIVES OF PHENYLBORIC ACID, THEIR PREPARATION AND ACTION UPON BACTERIA. II. HYDROXYPHENYLBORIC ACIDS1 , 1932 .