METHOD FOR MEASURING EFFECTIVENESS OF METALLOPROTENASE INHIBITOR ON MEDICAL TREATMENT, NEW INHIBITOR AND ITS USE ONMEDICAL TREATMENT

摘要

PROBLEM TO BE SOLVED: To provide a method for quantitatively and highly reliably evaluating the activity of a substance inhibiting an enzyme existing in snake venom and mammal body, and to obtain the inhibitor evaluated by the method. SOLUTION: (A) Using a zinc-dependent metalloproteinase existing in the venom of snakes belonging to Grotalidae or Viperidae, the inhibitory activity of a peptide analogue having ability to inhibit the above enzyme is subjected to primary screening. Subsequently, (B) the inhibitory activity of the above- mentioned peptide analogue against the zinc-dependent metalloproteinase existing in mammal body is assayed. Then, (C) the activity of the peptide analogue for a relevant morbid state is demonstrated by the standard pharmacological examination. The peptide analogue is e.g. a compound of formula I [A is a group of formula II; Y is OH, NH2 , NHOH, etc.; R4 is CH-(CH3 )2 , phenyl, etc.; X is 5-methoxy-1-indanon-3-acetyl, naphthoyl, etc.].