Mini-Reviews in Medicinal Chemistry

Author(s): Monika I. Konaklieva and Balbina J. Plotkin

DOI: 10.2174/1389557043403611

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The Relationship Between Inhibitors of Eukaryotic and Prokaryotic Serine Proteases

Page: [721 - 739] Pages: 19

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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 (betalactamases), 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.

Keywords: serine proteases, lactamases, human leukocyte elastase, serine protease inhibitors