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 | |
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 |