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  • Cinnamates and cinnamamides inhibit fungal 17ß-hydroxysteroid dehydrogenase
    Kristan, Katja, 1975- ...
    The 17ß-hydroxysteroid dehydrogenases (17ß-HSDs) have important roles in the regulation of steroid hormone actions through their catalysis of the oxidationor reduction of estrogens and androgens at ... position 17. Dysfunctions of the human 17Ž-HSDs have been associated with reproduction disorders, neuronal diseases and the development of hormone-dependent forms of cancers. Therefore, these enzymes represent interesting targets for the development of new drugs. Here we present a series of new cinnamic acid esters and amides that inhibit the oxidative and reductive reaction catalyzed by 17Ž-HSD from the fungus Cochliobolus lunatus, a model enzyme of the short-chain dehydrogenasežreductase superfamily. We found that esters of unsubstituted cinnamic acid were better inhibitors than esters of 3,4,5-trimethoxycinnamic acid. Cinnamates were also more potent inhibitors than structurally related cinnamamides. The compounds presented in this paper are potential leads for the development of inhibitors of human 17Ž-HSD isoforms, which may prove to have different therapeutic applications.
    Vir: The international workshop on 11beta and 17beta-hydroxysteroid dehydrogenases, Elmau Castle, 8-11 May 2005 (no. 1/2, 2006, str. 239-241)
    Vrsta gradiva - prispevek na konferenci
    Leto - 2006
    Jezik - angleški
    COBISS.SI-ID - 1900913

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