Mapping the extended substrate binding site of cathepsin G and human leukocyte elastase. Studies with peptide substrates related to the alpha 1-protease inhibitor reactive site.
Sbustrate specificity of the elastase and the chymotrypsin-like enzyme of the human granulocyte.
Direct fluorescent assay of urokinase and plasminogen activators of normal and malignant cells: kinetics and inhibitor profiles.
- M. Zimmerman, J. Quigley, B. Ashe, C. Dorn, R. Goldfarb, W. Troll
- BiologyProceedings of the National Academy of Sciences…
- 1 February 1978
A direct rate assay for plasminogen activator has been developed using a synthetic fluorogenic peptide substrate, 7-(N-Cbz-glycylglycylargininamido)-4-methylcoumarin trifluoroacetate, which should be useful for the study of the effect of various agents on functional changes in cells secreting this enzyme.
Cephalosporin antibiotics can be modified to inhibit human leukocyte elastase
It is reported that neutral cephalosporins (that is, compounds not bearing a free carboxyl at position C-4) can be modified to become potent time-dependent inhibitors of HLE.
Sensitive assays for trypsin, elastase, and chymotrypsin using new fluorogenic substrates.
Specific inhibition of human granulocyte elastase by cis-unsaturated fatty acids and activation by the corresponding alcohols.
Inhibition of human leukocyte elastase. 4. Selection of a substituted cephalosporin (L-658,758) as a topical aerosol.
While the most potent in vitro HLE inhibition had previously been obtained with lipophilic ester derivatives, it was found that the less active, but more polar and stable, amide derivatives were much more effective in vivo.
The Discovery and Biologic Properties of Cephalosporin‐Based Inhibitors of PMN Elastase
A failure to maintain normal levels of elastase and cathepsin G in mature PMNs in the beige mousezo has been described which may be due to inactivation of enzyme by inhibitors present.
Orally Active β‐Lactam Inhibitors of Human Leukocyte Elastase. Part 3. Stereospecific Synthesis and Structure‐Activity Relationships for 3,3‐Dialkylazetidin‐2‐ones.