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Review Article

Succinimide and Saccharin-based Enzyme-activated Inhibitors of Serine Proteases

[ Vol. 5 , Issue. 6 ]

Author(s):

Derek C. Martyn, Michael J.B. Moore and Andrew D. Abell   Pages 405 - 415 ( 11 )

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.

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