The relationship between inhibitors of eukaryotic and prokaryotic serine proteases.
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.
Konaklieva
Monika I
MI
Department of Chemistry, American University, Washington, DC 20016, USA. mkonak@american.edu
Plotkin
Balbina J
BJ
D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D005057:Eukaryotic Cells / Q000187:drug effects* / Q000201:enzymology; D006801:Humans; D015394:Molecular Structure; D010802:Phylogeny; D011387:Prokaryotic Cells / Q000187:drug effects* / Q000201:enzymology; D012697:Serine Endopeptidases / Q000737:chemistry / Q000378:metabolism*; D015842:Serine Proteinase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D065093:beta-Lactamase Inhibitors; D001618:beta-Lactamases / Q000737:chemistry
D000900:Anti-Bacterial Agents; D015842:Serine Proteinase Inhibitors; D065093:beta-Lactamase Inhibitors; D012697:Serine Endopeptidases; D001618:beta-Lactamases