17β-Hydroxysteroid Dehydrogenase Type 1 Inhibition: A Potential Treatment Option for Non-Small Cell Lung Cancer
| العنوان: | 17β-Hydroxysteroid Dehydrogenase Type 1 Inhibition: A Potential Treatment Option for Non-Small Cell Lung Cancer |
|---|---|
| المؤلفون: | 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 |
| المساهمون: | HIPS, Helmholtz-Institut für Pharmazeutische Forschung Saarland, Universitätscampus E8.1 66123 Saarbrücken, Germany. |
| المصدر: | 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 |
| بيانات النشر: | ACS, 2021. |
| سنة النشر: | 2021 |
| مصطلحات موضوعية: | business.industry, Organic Chemistry, Treatment options, medicine.disease, Biochemistry, Docking, respiratory tract diseases, Drug Discovery, Cancer research, Medicine, Non small cell, Hydroxysteroid dehydrogenase, business, Lung cancer, hormones, hormone substitutes, and hormone antagonists |
| الوصف: | [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 a viable target for treating this disease. Synthesis of a rationally designed library of 2,5-disubstituted furan derivatives followed by biological screening led to the discovery of 17β-HSD1 inhibitor 1, capable of fully inhibiting human NSCLC Calu-1 cell proliferation. Its pharmacological profile renders it eligible for further in vivo studies. The very high selectivity of 1 over 17β-HSD2 was investigated, revealing a rational approach for the design of selective inhibitors. 17β-HSD1 and 1 hold promise in fighting NSCLC. |
| اللغة: | English |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4b72b1eb9a0d3948ea61df325c6e341e https://hdl.handle.net/10033/623149 |
| حقوق: | OPEN |
| رقم الأكسشن: | edsair.doi.dedup.....4b72b1eb9a0d3948ea61df325c6e341e |
| قاعدة البيانات: | OpenAIRE |
| الوصف غير متاح. |