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

Non-animal skin sensitization safety assessments for cosmetic ingredients – What is possible today?

Autor: Daniel Neumann, Emanuele M. Gargano, Kimberly Zupko, Valerie Politano, Helga Rothe, Kirstin Kosemund-Meynen, Carsten Goebel, Sheppard Martin, Neelam Jaiswal, Jin Zhang, Gábor von Bölcshazy

Publikováno v: Current Opinion in Toxicology. 5:46-54

A key part of the safety assessment for cosmetic ingredients is the evaluation of skin sensitization, i.e. their potency to induce an immune response in the skin involving the innate and the adaptive immune system. For decades the murine local lymph

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::6b3efd8f942a0f77917234ff1e2079d4
https://doi.org/10.1016/j.cotox.2017.08.005

Discovery of a new class of bicyclic substituted hydroxyphenylmethanones as 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) inhibitors for the treatment of osteoporosis

Autor: Stefan Hinsberger, Rolf W. Hartmann, Emanuele M. Gargano, Marie Wetzel, Sandrine Marchais-Oberwinkler

Publikováno v: European Journal of Medicinal Chemistry. 47:1-17

E2 deficiency in elderly people has directly an effect on the skeleton and can lead to osteoporosis. As 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) catalyses the conversion between active 17β-hydroxysteroid estradiol (E2) and testosterone (

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::86d229ca07fca7e00a9c0489631e86e3
https://doi.org/10.1016/j.ejmech.2011.09.004

Addressing cytotoxicity of 1,4-biphenyl amide derivatives: Discovery of new potent and selective 17β-hydroxysteroid dehydrogenase type 2 inhibitors

Autor: Rolf W. Hartmann, Sandrine Marchais-Oberwinkler, Enrico Perspicace, Emanuele M. Gargano, Angelo Carotti

Publikováno v: Bioorganicmedicinal chemistry letters. 26(1)

Four different classes of new 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) inhibitors were synthesized, in order to lower the cytotoxicity exhibited by the lead compound A, via disrupting the linearity and the aromaticity of the biphenyl moie

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::de18324b6f126fe748b3d38b8516b4eb
https://pubmed.ncbi.nlm.nih.gov/26615885

Novel, potent and selective 17β-hydroxysteroid dehydrogenase type 2 inhibitors as potential therapeutics for osteoporosis with dual human and mouse activities

Autor: Nina Hanke, Emanuele M. Gargano, Enrico Perspicace, Rolf W. Hartmann, Sandrine Marchais-Oberwinkler, Angelo Carotti, Liliana Cozzoli

Publikováno v: European journal of medicinal chemistry. 83

17β-Hydroxysteroid dehydrogenase type 2 (17β-HSD2) is responsible for the oxidation of the highly active estradiol (E2) and testosterone (T) into the less potent estrone (E1) and Δ4-androstene-3,17-dione (Δ4-AD), respectively. As 17β-HSD2 is pre

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::58a74c144421a220184d9b0643de195e
https://pubmed.ncbi.nlm.nih.gov/24974351