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Discovery of Multi-Target Agents Active as Broad-Spectrum Antivirals and Correctors of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) for Associated Pulmonary Diseases.

Tassini, S; Sun, L; Lanko, K; Crespan, E; Langron, E; Falchi, F; Kissova, M; ... Radi, M; + view all (2017) Discovery of Multi-Target Agents Active as Broad-Spectrum Antivirals and Correctors of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) for Associated Pulmonary Diseases. Journal of Medicinal Chemistry 10.1021/acs.jmedchem.6b01521. (In press). Green open access

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Abstract

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 enterovirus 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 multi-target agents active both as broad-spectrum antivirals and as correctors of the F508del-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 enteroviruses representative of all major species.

Type: Article
Title: Discovery of Multi-Target Agents Active as Broad-Spectrum Antivirals and Correctors of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) for Associated Pulmonary Diseases.
Location: United States
Open access status: An open access version is available from UCL Discovery
DOI: 10.1021/acs.jmedchem.6b01521
Publisher version: http://dx.doi.org/10.1021/acs.jmedchem.6b01521
UCL classification: UCL > Provost and Vice Provost Offices
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > Div of Biosciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > Div of Biosciences > Neuro, Physiology and Pharmacology
URI: http://discovery.ucl.ac.uk/id/eprint/1537559
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