Document Detail

Succinimide and saccharin-based enzyme-activated inhibitors of serine proteases.
MedLine Citation:
PMID:  10390606     Owner:  NLM     Status:  MEDLINE    
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.
D C Martyn; M J Moore; A D Abell
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Review    
Journal Detail:
Title:  Current pharmaceutical design     Volume:  5     ISSN:  1381-6128     ISO Abbreviation:  Curr. Pharm. Des.     Publication Date:  1999 Jun 
Date Detail:
Created Date:  1999-08-12     Completed Date:  1999-08-12     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9602487     Medline TA:  Curr Pharm Des     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  405-15     Citation Subset:  IM    
Department of Chemistry, University of Canterbury, Christchurch, New Zealand.
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MeSH Terms
Binding Sites
Leukocyte Elastase / antagonists & inhibitors*
Saccharin / pharmacology*
Serine Proteinase Inhibitors / pharmacology*
Structure-Activity Relationship
Succinimides / pharmacology*
Reg. No./Substance:
0/Serine Proteinase Inhibitors; 0/Succinimides; 123-56-8/succinimide; 81-07-2/Saccharin; EC Elastase

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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