[Screening, characterization and pharmaceutical and medical application of enzyme inhibitors from microbial origin...

In living organisms a large number of enzymes are working in complicated networks to express various biological functions. In order to analyze such functions from various aspects, specific enzyme inhibitors are likely to become useful tools. They are also useful for the studies of reaction mechanisms and analysis of three-dimensional structures of enzymes. Moreover, they are of great value in elucidating disease processes and seem to have usefulness in treatment of various diseases. Searching for inhibitors in culture filtrate of microbes, we discovered many substances which specifically inhibit various enzymes such as endopeptidases, exopeptidases, glycosidases, lipases, an so forth. These inhibitors have low-molecular-weights and unique structures. We found significant activities of exopeptidases, alkaline phosphatases, esterases, and so forth, on surface membranes of various mammalian cells. Searching for specific inhibitors against these cell surface enzymes, we have discovered many interesting inhibitors. These inhibitors proved to bind to the cellular surface and to modify the functions of cells involved in immune responses. Thus the studies on these enzyme inhibitors may well afford important keys to understand various aspect of biological phenomena and diseases: inflammation, immune response, hypertension, hyperlipemia, diabetes, Alzheimer's disease, carcinogenesis, metastasis, viral infection, autoimmune diseases, and so forth. Because of their interesting pharmacological activities, some of the inhibitors are now under clinical evaluation for their uses as medical drugs. Enzyme inhibitors seems to propose a new promising field of science.