Studies of MR 889, a new synthetic proteinase inhibitor.
We investigated the proteinase inhibitory activity of MR 889, a thiolactic acid derivative. It is able to in vitro inhibit at low concentration (10(-5),10(-6)M) the activity of porcine pancreatic elastase, human neutrophil elastase and bovine chymotrypsin. In addition, MR 889 is able to inhibit the residual activity of alpha 2-macroglobulin-trapped human neutrophil elastase, paralleling the efficacy of phenylmethylsufonylfluoride. Finally, MR 889 has been shown to in vitro reduce the burden of elastase- and chymotrypsin-like activity found in sputum sol-phases of patients admitted for chronic bronchitis exacerbation.
Luisetti
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M
Istituto di Tisiologia e Malattie Respiratorie dell'Università, IRCCS Policlinico San Matteo, Pavia, Italy.
Piccioni
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PD
Donnini
M
M
Peona
V
V
Pozzi
E
E
Grassi
C
C
D002918:Chymotrypsin / Q000037:antagonists & inhibitors; D006801:Humans; D007700:Kinetics; D010196:Pancreatic Elastase / Q000037:antagonists & inhibitors; D011480:Protease Inhibitors / Q000494:pharmacology*; D013183:Sputum / Q000201:enzymology; D013876:Thiophenes / Q000494:pharmacology*
D011480:Protease Inhibitors; D013876:Thiophenes; C062051:midesteine; D002918:Chymotrypsin; D010196:Pancreatic Elastase