METHOD FOR PRODUCING DERIVATIVES OF CHYMOTRYPSIN-TRYPSIN-LIKE PROTEOLITYC ENZYMES SUITABLE FOR PARENTERAL ADMINISTRATION

摘要

The invention relates to the method for producing the derivatives of chymotrypsin-trypsin-like proteolityc enzymes comprising the inactivation of the hydrolytic center of the enzyme. The inactivation is provided chemically or by the mutagenic substitution of the amino acid residues comprising the "proton relay" of the enzyme corresponding to histidine-57, aspartic acid-102 and serine-195 (according to the amino acid sequence of a- chymotrypsin). As a result, the derivative is devoid of the hydrolytic activity, while the structure and the binding properties are kept intact. Such a preparation is suitable for parenteral administration. The preparation may be used as a means for the tissue proteolysis possessing low toxicity and low immunogenicity.