M
Marie Wetzel
Researcher at Saarland University
Publications - 9
Citations - 401
Marie Wetzel is an academic researcher from Saarland University. The author has contributed to research in topics: Hydroxysteroid dehydrogenase & Estrogen. The author has an hindex of 8, co-authored 9 publications receiving 370 citations.
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Journal ArticleDOI
17β-Hydroxysteroid dehydrogenases (17β-HSDs) as therapeutic targets: protein structures, functions, and recent progress in inhibitor development.
Sandrine Marchais-Oberwinkler,Claudia Henn,Gabriele Möller,Tobias Klein,Matthias Negri,Alexander Oster,Alessandro Spadaro,Ruth Werth,Marie Wetzel,Kuiying Xu,Martin Frotscher,Rolf W. Hartmann,Jerzy Adamski +12 more
TL;DR: An overview of functional and structural aspects for the different 17β-HSDs is given and the selective inhibition of the concerned enzymes might provide an effective treatment and a good alternative to the existing endocrine therapies.
Journal ArticleDOI
New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17β-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of estrogen-dependent diseases.
Sandrine Marchais-Oberwinkler,Marie Wetzel,Erika Ziegler,Patricia Kruchten,Ruth Werth,Claudia Henn,Rolf W. Hartmann,Martin Frotscher +7 more
TL;DR: Inhibition of 17β-HSD1 inhibitors from the hydroxyphenylnaphthol class by introduction of different heteroaromatic rings as well as substituted phenyl groups showed a good membrane permeation and metabolic stability and was orally available in the rat.
Journal ArticleDOI
17β-HSD2 inhibitors for the treatment of osteoporosis: Identification of a promising scaffold
TL;DR: Inhibition of 17β-HSD2 may provide a new and promising approach to prevent the onset of osteoporosis, keeping a certain level in estrogens and androgens in bone cells of ageing people.
Journal ArticleDOI
Introduction of an electron withdrawing group on the hydroxyphenylnaphthol scaffold improves the potency of 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) inhibitors.
Marie Wetzel,Sandrine Marchais-Oberwinkler,Enrico Perspicace,Gabriele Möller,Jerzy Adamski,Rolf W. Hartmann +5 more
TL;DR: Compound 19 turned out to be the most potent and selective inhibitor of 17 β-HSD2 in cell-free assays and had a very good cellular activity in MDA-MB-231 cells, expressing naturally 17β- HSD2.
Journal ArticleDOI
Discovery of a new class of bicyclic substituted hydroxyphenylmethanones as 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) inhibitors for the treatment of osteoporosis.
Marie Wetzel,Emanuele M. Gargano,Stefan Hinsberger,Sandrine Marchais-Oberwinkler,Rolf W. Hartmann +4 more
TL;DR: Highly selective compounds (11, 12, 14, 21 and 22) have been identified, the most promising one (12) showing an IC(50) value in the low nanomolar range (101 nM) and a selectivity factor of 13 toward 17β-HSD1 and an interesting candidate for further biological evaluation.