Author/Editor     Kristan, Katja; Starčević, Štefan; Brunskole, Mojca; Lanišnik-Rižner, Tea; Gobec, Stanislav
Title     Cinnamates and cinnamamides inhibit fungal 17beta-hydroxysteroid dehydrogenase
Type     članek
Source     Mol Cell Endocrinol
Vol. and No.     Letnik 248, št. 1-2
Publication year     2006
Volume     str. 239-41
ISSN     0303-7207
Language     eng
Abstract     The 17beta-hydroxysteroid dehydrugenases (17beta-HSDs) have important roles in the regulation of steroid hormone actions through their catalysis of the oxidation or reduction of estrogens and androgens at position 17. Dysfunctions of the human 17beta-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 und reductive reaction catalyzed hy 17beta-HSD from the tungus Cochliobolus lunatus, a model enzyme of the short-chain dehydrogenase/reductase 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 polential leads for the development of inhibitors of human 17beta-HSD isoforms, which may prove to have different therapeutic applications.
Descriptors     17-HYDROXYSTEROID DEHYDROGENASES
ASCOMYCETES
ENZYME INHIBITORS
CINNAMATES