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Searching for inhibitors of fungal 17ß-hydroxysteroid dehydrogenaseKristan, Katja, 1975- ...17beta-Hydroxysteroid dehydrogenases (17(beta-HSDs) have key roles in hormonalregulation and function in the human, and as such they represent emerging therapeutic targets for the control of ... estrogen- and androgen-dependent diseases. Our model enzyme is 17beta-HSD from the fungus Cochliobolus lunatus 17(beta-HSDcI), and we have used different approaches to find potent inhibitors of this enzyme. Using "classical" inhibition assays, wehave shown that some phytoestrogens and cinnamic acid esters are potent in their inhibition of the oxidation of 4-estrene-17beta-o1-3-one and the reduction of 4estrene-3,17-dione catalyzed by 17beta-HSDcI. We have also examined peptides as potential inhibitors of 17beta-HSDcI on the basis that this enzyme is a homodimer under native conditions. Thus, compounds that specifically prevent the formation of dimers could represent a new class of inhibitors, since dimerization is a prerequisite for catalysis. We have shown that a 33-amino-acid-long peptide binds to the dimerization surface, prevents the formation of dimers, and consequently inhibits 17betaHSDcI. Finally, we also show that phage display provides another tool in the search for inhibitors that bind to the surface or in the active site of 17betaH SDcI.Source: Enzymology and molecular biology of carbonyl metabolism 13 (Str. 263-272)Type of material - article, component partPublish date - 2007Language - englishCOBISS.SI-ID - 22664153
Author
Kristan, Katja, 1975- |
Sova, Matej, 1979- |
Lunder, Mojca, 1977- |
Bratkovič, Tomaž, farmacevt, 1978- |
Gobec, Stanislav, 1970- |
Štrukelj, Borut |
Stojan, Jure, 1956- |
Adamski, Jerzy, molekularna biologija |
Lanišnik-Rižner, Tea
Topics
17-Hydroxysteroid Dehydrogenases |
Enzyme Inhibitors |
Ascomycetes |
Enzymology |
Estrogens |
17-hidroksisteroidne dehidrogenaze |
Encimski inhibitorji |
Estrogeni
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Kristan, Katja, 1975- | 24392 |
Sova, Matej, 1979- | 25490 |
Lunder, Mojca, 1977- | 25096 |
Bratkovič, Tomaž, farmacevt, 1978- | 23598 |
Gobec, Stanislav, 1970- | 15284 |
Štrukelj, Borut | 07849 |
Stojan, Jure, 1956- | 03723 |
Adamski, Jerzy, molekularna biologija | 55378 |
Lanišnik-Rižner, Tea | 11699 |
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