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1. Succinimide and saccharin-based enzyme-activated inhibitors of serine proteases.

Author

Martyn DC, Moore MJ, and Abell AD

Subjects
Binding Sites, Humans, Structure-Activity Relationship, Leukocyte Elastase antagonists & inhibitors, Saccharin pharmacology, Serine Proteinase Inhibitors pharmacology, Succinimides pharmacology
Abstract

The inhibition of human leukocyte elastase (HLE), and other serine proteases, by succinimide and saccharin-based compounds is reviewed. The succinimide compounds are unique in that the inactivating species is generated within the enzyme active site via a molecular rearrangement. The related saccharin derivatives also inactivate serine proteases by an enzyme-activated mechanism. Those factors effecting the potency, selectivity and stability of these important classes of inhibitor are discussed.

Published
1999

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