Title: The inhibition of human neutrophil elastase and cathepsin G by peptidyl 1,2-dicarbonyl derivatives
Abstract: Neutrophil elastase and cathepsin G are serine proteases that can damage connective tissue and trigger other pathological reactions. Compounds containing a peptide sequence to impart specificity and bearing an α-dicarbonyl unit (α-diketone or α-keto ester) at the carboxy terminus are potent inhibitors of the neutrophil serine proteases (human neutrophil elastase: R-Val-COCH3, Ki = 0.017 μM; R-Val-COOCH3, Ki = 0.002 μM; human neutrophil cathepsin G: R-Phe-COCH3, Ki = 0.8 μM; R-Phe-COOCH3, Ki = 0.44 μM; R = N-(4-[(4-chlorophenyl)sulfonylaminocarbonyl]phenylcarbonyl)ValylProlyl).
Publication Year: 1990
Publication Date: 1990-01-01
Language: en
Type: article
Indexed In: ['crossref', 'pubmed']
Access and Citation
Cited By Count: 27
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