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

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

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

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

Treatment of estrogen-dependent diseases: Design, synthesis and profiling of a selective 17β-HSD1 inhibitor with sub-nanomolar IC 50 for a proof-of-principle study

Autor: Emmanuel Bey, Chris J. van Koppen, Matthias W. Laschke, Mohamed Salah, Carsten Börger, Martin Frotscher, Ahmed S. Abdelsamie, Lorenz Siebenbürger, Michael D. Menger

Publikováno v: European Journal of Medicinal Chemistry. 127:944-957

Current endocrine therapeutics for the estrogen-dependent disease endometriosis often lead to considerable side-effects as they act by reducing estrogen action systemically. A more recent approach takes advantage of the fact that the weak estrogen es

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::681b60c43a98312f9761a0d03b45cfb3
https://doi.org/10.1016/j.ejmech.2016.11.004