Elastases biological inhibitors

Fluorinated /1-Lactams and Biological Activities of /f-Lactamase and Elastase Inhibitors ... 

Very recently, (3-lactam antibiotics have been shown to offer neuroprotection by increasing glutamate transporters expression via gene activation [15] in addition, the discoveries of new biologically active (3-lactams such as cholesterol acyl transferase inhibitors [16-18], thrombin inhibitors [19], human cytomegalovirus protease inhibitors [20], matrix-metallo protease inhibitors [21], inhibitors of human leukocyte elastase (HLE) [22, 23] and cysteine protease [24, 25], and apoptosis inductors [26, 27] have provided much needed motivation for continuous development of new (3-lactam systems. 

All human cystatins are assumed to have major biological roles as inhibitors of one or more target proteases of human and/or nonhuman origin. Identification of target proteases of biomedical relevance is, however, difficult. Only few examples of clear-cut identifications of target proteases for inhibitors are known, and these identifications usually rely on experiments by Nature and not by Man. Two examples are the identifications of granulocyte elastase as a target enzyme... 

Shi, Y., and Sharma, S. (1999) Metallopep-tide approach to the design of biologically active ligands Design of specific human neutrophil elastase inhibitors. Bioorg. Med. Chem. Lett. 9, 1469-1474. 

Smith, D., Kirschenheuter, G.R, Charlton, J., Guidot, D.M., and Repine, J.E. In vitro selection of RNA-based irreversible inhibitors of human neutrophil elastase. Chemistry and Biology 2,741-750,1995. 

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