4D-QSAR Study of 17β-Hydroxysteroid Dehydrogenase Type 3 Inhibitors
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چکیده
منابع مشابه
Hydroxybenzothiazoles as New Nonsteroidal Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1)
17β-estradiol (E2), the most potent estrogen in humans, known to be involved in the development and progession of estrogen-dependent diseases (EDD) like breast cancer and endometriosis. 17β-HSD1, which catalyses the reduction of the weak estrogen estrone (E1) to E2, is often overexpressed in breast cancer and endometriotic tissues. An inhibition of 17β-HSD1 could selectively reduce the local E2...
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s: I. Wölfling J, Bóna Á, Frank É, Schneider G, Berényi Á, Zupkó I. Synthesis and cytotoxic activity of 16-benzylidene estrone 3-methyl ethers. Hungarian-AustrianCzech-German-Greek-Italian-Polish-Slovak-Slovenian Joint Meeting on Medicinal Chemistry, 24-27. June, 2009, Budapest, Hungary. II. Zupkó I, Berényi Á, Marchais-Oberwinkler S, Frotscher M. Direct antiproliferative effect of novel nonste...
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17β-Hydroxysteroid dehydrogenase type 10 (17β-HSD10) is encoded by the HSD17B10 gene mapping at Xp11.2. This homotetrameric mitochondrial multifunctional enzyme catalyzes the oxidation of neuroactive steroids and the degradation of isoleucine. This enzyme is capable of binding to other peptides, such as estrogen receptor α, amyloid-β, and tRNA methyltransferase 10C. Missense mutations of the HS...
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The steroid hormones are lipophilic compounds with low molecular weight, derived from cholesterol, which play a crucial role in differentiation, development and physiological functions of many tissues. They are synthesized primarily by endocrine glands, such as the gonads, the adrenal glands and the feto-placental unit during pregnancy. In addition, the central nervous system (CNS) seems to be ...
متن کاملStructural Basis for Species Specific Inhibition of 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Computational Study and Biological Validation
17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) catalyzes the reduction of estrone to estradiol, which is the most potent estrogen in humans. Inhibition of 17β-HSD1 and thereby reducing the intracellular estradiol concentration is thus a promising approach for the treatment of estrogen dependent diseases. In the past, several steroidal and non-steroidal inhibitors of 17β-HSD1 have been descr...
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ژورنال
عنوان ژورنال: Journal of the Brazilian Chemical Society
سال: 2019
ISSN: 0103-5053
DOI: 10.21577/0103-5053.20190052