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The Importance of Correct Protein Concentration for Kinetics and Affinity Determination in Structure-function Analysis
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The relationship between inhibitors of eukaryotic and prokaryotic serine proteases
Monika I Konaklieva1, Balbina J Plotkin
1Department of Chemistry, American University, Washington, DC 20016, USA. mkonak@american.edu
Abstract:
The ability to inhibit serine proteases is a major focus in the pharmaceutical industry. Serine proteases of medical importance range in phylogenetic diversity from the metallo-proteases, which play a role in pulmonary hypertension, and destruction of the lung parenchyma in emphysema, to those proteases (beta-lactamases), which play a role in the resistance of bacteria to beta-lactam antibiotics. In both the mammalian and microbial systems, the development of serine protease inhibitors has been a focal strategy spurring investigations in the area of serine protease dependent prodrugs that incorporate a bactericidal moiety as well as other classes of metalloprotease inhibitors.
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