Assay for evaluating inhibition of PMN elastase by N-substituted

Chemistry: molecular biology and microbiology – Measuring or testing process involving enzymes or... – Involving antigen-antibody binding – specific binding protein...

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435 18, 435 23, 435218, 435184, C12Q 137, C12Q 966, G01N 3353, C12N 999

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052292673

ABSTRACT:
N-substituted azetidinones are a class of inhibitors of human leukocytes elastase which are known to be useful in the treatment of a wide variety of antiinflammatory and antidegenerative diseases. In inhibiting elastase, the therapeutic agents are shown to form a characteristic stable complex with the enzyme. In the assay disclosed herein, the inhibitor-enzyme complex is advantageously hydrolyzed and specific product(s) of the hydrolysis are measured. The assays are useful in a clinical setting, for determining appropriate dosage and assessing the effectiveness of treatment.

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Jaenicke et al in Protein Structure a Practical Approach pp. 191-223 (1990).
Colman in Protein Function A Practical Approach pp. 77-99 (1990).
Rando Meth. Enz. 46 pp. 28-41 (1977).
Chem Abstracts, vol. 78, No. 17, 30 Apr. 1973.
Chem Abstracts, vol. 115, No. 13, 30 Sep. 1991.

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