Výsledky vyhledávání - "Martin Frotscher"

Akademický článek

17β-Hydroxysteroid Dehydrogenase Type 2 Inhibition: Discovery of Selective and Metabolically Stable Compounds Inhibiting Both the Human Enzyme and Its Murine Ortholog.

Autor: Emanuele M Gargano, Giuseppe Allegretta, Enrico Perspicace, Angelo Carotti, Chris Van Koppen, Martin Frotscher, Sandrine Marchais-Oberwinkler, Rolf W Hartmann

Publikováno v: PLoS ONE, Vol 10, Iss 7, p e0134754 (2015)

Design and synthesis of a new class of inhibitors for the treatment of osteoporosis and its comparative h17β-HSD2 and m17β-HSD2 SAR study are described. 17a is the first compound to show strong inhibition of both h17β-HSD2 and m17β-HSD2, intracel

Externí odkaz: https://doaj.org/article/0bc4d2b54c854517a63ff00bf9fcb5c9

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Akademický článek

Hydroxybenzothiazoles as new nonsteroidal inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1).

Autor: Alessandro Spadaro, Matthias Negri, Sandrine Marchais-Oberwinkler, Emmanuel Bey, Martin Frotscher

Publikováno v: PLoS ONE, Vol 7, Iss 1, p e29252 (2012)

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 e

Externí odkaz: https://doaj.org/article/8b5b42ff1bff47bcaee02bfde7a2d7c2

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Akademický článek

Structural basis for species specific inhibition of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1): computational study and biological validation.

Autor: Tobias Klein, Claudia Henn, Matthias Negri, Martin Frotscher

Publikováno v: PLoS ONE, Vol 6, Iss 8, p e22990 (2011)

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 promis

Externí odkaz: https://doaj.org/article/45cc11ccb04c4095995648f3d3a5c1df

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Dual Targeting of Steroid Sulfatase and 17β-Hydroxysteroid Dehydrogenase Type 1 by a Novel Drug-Prodrug Approach: A Potential Therapeutic Option for the Treatment of Endometriosis

Autor: Abdelrahman Mohamed, Mohamed Salah, Mariam Tahoun, Manuel Hawner, Ahmed S. Abdelsamie, Martin Frotscher

Publikováno v: Journal of medicinal chemistry. 65(17)

A novel approach for the dual inhibition of steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1(17β HSD1) by a single drug was explored, starting from in-house 17β HSD1 inhibitors via masking their phenolic OH group with a sulfamat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::16cdeffc24d89f049400a1ed565610da
https://pubmed.ncbi.nlm.nih.gov/35993890

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17β-Hydroxysteroid Dehydrogenase Type 1 Inhibition: A Potential Treatment Option for Non-Small Cell Lung Cancer

Autor: Rolf W. Hartmann, Chris J. van Koppen, Matthias W. Laschke, Giuseppe Felice Mangiatordi, Ahmed S. Abdelsamie, Martin Frotscher, Orazio Nicolotti, Abdelrahman Mohamed, Angelo Carotti, Arcangela Mazzini, Hanna Drzewiecka, Emanuele M. Gargano, Paweł P. Jagodziński, Sandrine Marchais-Oberwinkler

Publikováno v: ACS medicinal chemistry letters
United States
ACS Med Chem Lett
ACS medicinal chemistry letters (2021). doi:10.1021/acsmedchemlett.1c00462
info:cnr-pdr/source/autori:Emanuele M. Gargano, Abdelrahman Mohamed, Ahmed S. Abdelsamie, Giuseppe F. Mangiatordi, Hanna Drzewiecka, Pawe? P. Jagodzi?ski, Arcangela Mazzini, Chris J. van Koppen, Matthias W. Laschke, Orazio Nicolotti, Angelo Carotti, Sandrine Marchais-Oberwinkler, Rolf W. Hartmann, and Martin Frotscher/titolo:17?-Hydroxysteroid Dehydrogenase Type 1 Inhibition: A Potential Treatment Option for Non-Small Cell Lung Cancer/doi:10.1021%2Facsmedchemlett.1c00462/rivista:ACS medicinal chemistry letters/anno:2021/pagina_da:/pagina_a:/intervallo_pagine:/volume

[Image: see text] In the face of the clinical challenge posed by non-small cell lung cancer (NSCLC), the present need for new therapeutic approaches is genuine. Up to now, no proof existed that 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) is

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4b72b1eb9a0d3948ea61df325c6e341e
https://hdl.handle.net/10033/623149

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A Hybrid In Silico/In Vitro Target Fishing Study to Mine Novel Targets of Urolithin A and B: A Step Towards a Better Comprehension of Their Estrogenicity

Autor: Margherita Interlandi, Angela Falco, Paola Puccini, Benedetta Riccardi, Chiara Dall'Asta, Abdelrahman Mohamed, Martin Frotscher, Daniele Del Rio, Marco Milioli, Luca Dellafiora, Gianni Galaverna

Publikováno v: Molecular nutritionfood research. 64(16)

Scope Urolithin A and B are gut metabolites of ellagic acid and ellagitannins associated with many beneficial effects. Evidence in vitro pointed to their potential as estrogenic modulators. However, both molecular mechanisms and biological targets in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::28e38d730a0c40db8edbf0a574574976
https://pubmed.ncbi.nlm.nih.gov/32640069

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Highly Potent 17β-HSD2 Inhibitors with a Promising Pharmacokinetic Profile for Targeted Osteoporosis Therapy

Autor: Lorenz Siebenbuerger, Sandrine Marchais-Oberwinkler, Michael D. Menger, Martin Frotscher, Ahmed S. Abdelsamie, Carsten Boerger, Rolf W. Hartmann, Victor Hernandez-Olmos, Claudia Scheuer, Chris J. van Koppen, Matthias W. Laschke

Publikováno v: Journal of Medicinal Chemistry. 61:10724-10738

Intracellular elevation of E2 levels in bone by inhibition of 17β hydroxysteroid dehydrogenase type 2 (17β-HSD2) without affecting systemic E2 levels is an attractive approach for a targeted therapy against osteoporosis, a disease which is characte

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c3a7ff0cde1f64d87d00e9445907fc28
https://doi.org/10.1021/acs.jmedchem.8b01373

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First Dual Inhibitors of Steroid Sulfatase (STS) and 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Designed Multiple Ligands as Novel Potential Therapeutics for Estrogen-Dependent Diseases

Autor: Ahmed S. Abdelsamie, Mohamed Salah, Martin Frotscher

Publikováno v: Journal of Medicinal Chemistry. 60:4086-4092

STS and 17β-HSD1 are attractive targets for the treatment of estrogen-dependent diseases like endometriosis and breast cancer. The simultaneous inhibition of both enzymes appears more promising than blockage of either protein alone. We describe a de

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9ab7539bb25c3ef750bb4e58e019a8ef
https://doi.org/10.1021/acs.jmedchem.7b00062

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Synthesis, anti-17β-HSD and antiproliferative activity of new substituted 5-nitrosopyrimidine analogs

Autor: Najim A. Al-Masoudi, Nabeel A. Abdul-Rida, Martin Frotscher, Tiba I. Mohammed

Publikováno v: Medicinal Chemistry Research. 26:830-840

A new series of 2-amino-4-alkylamino-6-methylamino-5-nitrosopyrimidine derivatives 10–14 have been synthesized from 5-nitrosopyrimidine analog 9 by nucleophilic aromatic substitution reaction with various amines using dimethylformamide as a solvent

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::7e3bba056fadf765e4322b5af8d44d76
https://doi.org/10.1007/s00044-017-1795-z

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