1996
DOI: 10.1007/bf02252944
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Abstract: The serine proteinases elastase and cathepsin G from polymorphonuclear granulocytes play a critical role in articular cartilage degradation, not only as proteolytic enzymes able to degrade the extracellular matrix but also by additionally modulating the level of active matrix metalloproteinases, key enzymes of the proteolytic destruction of cartilage during rheumatoid arthritis. The aim of our study was to examine whether anti-inflammatory drugs and selected compounds inhibited elastase and cathepsin G, and al… Show more

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Cited by 7 publications
(3 citation statements)
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“…A member of the potato inhibitor I family of serine protease inhibitors, this cysteine-free 8.1-kDa protein is a potent leukocyte elastase and cathepsin G inhibitor (Seemü ller et al, 1980;Schneibli et al, 1985). At one time, eglin was under serious consideration for drug development in light of it variously protecting against experimental models of emphysema, blocking neutrophil-mediated platelet aggregation, and inhibiting arthriticlike collagen degradation at very low doses (Lai and Diamond, 1990;Renesto et al, 1990;Steinmeyer and Kalbhen, 1996). Human trials were abandoned in the face of allergenicity and anaphylaxis (Schneibli and Liersch, 1989;Metz and Peet, 1999;Scheneibli, 2006).…”
Section: Eglinmentioning
confidence: 99%
“…A member of the potato inhibitor I family of serine protease inhibitors, this cysteine-free 8.1-kDa protein is a potent leukocyte elastase and cathepsin G inhibitor (Seemü ller et al, 1980;Schneibli et al, 1985). At one time, eglin was under serious consideration for drug development in light of it variously protecting against experimental models of emphysema, blocking neutrophil-mediated platelet aggregation, and inhibiting arthriticlike collagen degradation at very low doses (Lai and Diamond, 1990;Renesto et al, 1990;Steinmeyer and Kalbhen, 1996). Human trials were abandoned in the face of allergenicity and anaphylaxis (Schneibli and Liersch, 1989;Metz and Peet, 1999;Scheneibli, 2006).…”
Section: Eglinmentioning
confidence: 99%
“…Since the structure of a molecule plays an important role in its biological activity, this different kind of ligand-protein interaction could also be connected with the different pharmacological properties of these compounds. In fact, 5P5P and its hydroxy derivatives have good anticonvulsant properties and are used for the treatment of grand mal epilepsy; 7 in contrast, PHBUT is used therapeutically as an anti-inflammatory and anti-rheumatic drug 31,32 and 5M5P is much less effective than phenytoin derivatives containing two phenyl groups in the C-5 position of the 2,4-imidazolidinedione ring. 33 This possible structure-activity relationship is in line with the stereochemical requirements suggested for anticonvulsant drug action.…”
Section: Resultsmentioning
confidence: 99%
“…Insufficient levels of protease inhibitors has been therefore suggested as a contributing factor in a number of diseases including, among others, acute lung injury [2, 4, 5,], cystic fibrosis [6], ischemic reperfusion injury [7], rheumatoid arthritis [8], atherosclerosis [9], psoriasisT T [10] , and malignant tumors [11,12]. Moreover alpha-1 antitrypsin (α 1 -proteinase inhibitor) deficiency, an inherited disease, affects the lung and the liver.…”
Section: Introductionmentioning
confidence: 99%