Discovery of Multitarget Agents Active as Broad-Spectrum Antivirals and Correctors of Cystic Fibrosis Transmembrane Conductance Regulator for Associated Pulmonary Diseases
Enteroviruses (EVs) are among the most frequent infectious agents in humans worldwide and represent the leading cause of upper respiratory tract infections. No drugs for the treatment of EV infections are currently available. Recent studies have also linked EV infection with pulmonary exacerbations, especially in cystic fibrosis (CF) patients, and the importance of this link is probably underestimated. The aim of this work was to develop a new class of multitarget agents active both as broad-spectrum antivirals and as correctors of the F508del-cystic fibrosis transmembrane conductance regulator (CFTR) folding defect responsible for >90% of CF cases. We report herein the discovery of the first small molecules able to simultaneously act as correctors of the F508del-CFTR folding defect and as broad-spectrum antivirals against a panel of EVs representative of all major species.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2017 |
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| Erschienen: |
2017 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:60 |
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| Enthalten in: |
Journal of medicinal chemistry - 60(2017), 4 vom: 23. Feb., Seite 1400-1416 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Tassini, Sabrina [VerfasserIn] |
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| Links: |
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| Themen: |
126880-72-6 |
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| Anmerkungen: |
Date Completed 16.06.2017 Date Revised 04.11.2018 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1021/acs.jmedchem.6b01521 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM268332851 |
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| 520 | |a Enteroviruses (EVs) are among the most frequent infectious agents in humans worldwide and represent the leading cause of upper respiratory tract infections. No drugs for the treatment of EV infections are currently available. Recent studies have also linked EV infection with pulmonary exacerbations, especially in cystic fibrosis (CF) patients, and the importance of this link is probably underestimated. The aim of this work was to develop a new class of multitarget agents active both as broad-spectrum antivirals and as correctors of the F508del-cystic fibrosis transmembrane conductance regulator (CFTR) folding defect responsible for >90% of CF cases. We report herein the discovery of the first small molecules able to simultaneously act as correctors of the F508del-CFTR folding defect and as broad-spectrum antivirals against a panel of EVs representative of all major species | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 7 | |a Antiviral Agents |2 NLM | |
| 650 | 7 | |a Small Molecule Libraries |2 NLM | |
| 650 | 7 | |a Cystic Fibrosis Transmembrane Conductance Regulator |2 NLM | |
| 650 | 7 | |a 126880-72-6 |2 NLM | |
| 700 | 1 | |a Sun, Liang |e verfasserin |4 aut | |
| 700 | 1 | |a Lanko, Kristina |e verfasserin |4 aut | |
| 700 | 1 | |a Crespan, Emmanuele |e verfasserin |4 aut | |
| 700 | 1 | |a Langron, Emily |e verfasserin |4 aut | |
| 700 | 1 | |a Falchi, Federico |e verfasserin |4 aut | |
| 700 | 1 | |a Kissova, Miroslava |e verfasserin |4 aut | |
| 700 | 1 | |a Armijos-Rivera, Jorge I |e verfasserin |4 aut | |
| 700 | 1 | |a Delang, Leen |e verfasserin |4 aut | |
| 700 | 1 | |a Mirabelli, Carmen |e verfasserin |4 aut | |
| 700 | 1 | |a Neyts, Johan |e verfasserin |4 aut | |
| 700 | 1 | |a Pieroni, Marco |e verfasserin |4 aut | |
| 700 | 1 | |a Cavalli, Andrea |e verfasserin |4 aut | |
| 700 | 1 | |a Costantino, Gabriele |e verfasserin |4 aut | |
| 700 | 1 | |a Maga, Giovanni |e verfasserin |4 aut | |
| 700 | 1 | |a Vergani, Paola |e verfasserin |4 aut | |
| 700 | 1 | |a Leyssen, Pieter |e verfasserin |4 aut | |
| 700 | 1 | |a Radi, Marco |e verfasserin |4 aut | |
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