2. Academic Validation
  3. Discovery of Multitarget Agents Active as Broad-Spectrum Antivirals and Correctors of Cystic Fibrosis Transmembrane Conductance Regulator for Associated Pulmonary Diseases

Discovery of Multitarget Agents Active as Broad-Spectrum Antivirals and Correctors of Cystic Fibrosis Transmembrane Conductance Regulator for Associated Pulmonary Diseases

  • J Med Chem. 2017 Feb 23;60(4):1400-1416. doi: 10.1021/acs.jmedchem.6b01521.
Sabrina Tassini 1,  Liang Sun 2,  Kristina Lanko 2,  Emmanuele Crespan 3,  Emily Langron 4,  Federico Falchi 5 6,  Miroslava Kissova 3,  Jorge I Armijos-Rivera 3,  Leen Delang 2,  Carmen Mirabelli 2,  Johan Neyts 2,  Marco Pieroni 1,  Andrea Cavalli 5 6,  Gabriele Costantino 1,  Giovanni Maga 3,  Paola Vergani 4,  Pieter Leyssen 2,  Marco Radi 1
Affiliations

Affiliations

  • 1 P4T Group, Dipartimento di Scienze degli Alimenti e del Farmaco, Università degli Studi di Parma , Viale delle Scienze, 27/A, 43124 Parma, Italy.
  • 2 Laboratory of Virology and Experimental Chemotherapy, Rega Institute for Medical Research, KU Leuven , Minderbroedersstraat 10, 3000, Leuven, Belgium.
  • 3 Istituto di Genetica Molecolare , IGM-CNR, Via Abbiategrasso 207, 27100 Pavia, Italy.
  • 4 Department of Neuroscience, Physiology and Pharmacology, University College London , Gower Street, WC1E 6BT London, U.K.
  • 5 CompuNet, Istituto Italiano di Tecnologia , Via Morego 30, I-16163 Genova, Italy.
  • 6 Department of Pharmacy and Biotechnology, University of Bologna , Via Belmeloro 6, I-40126 Bologna, Italy.
PMID: 28122178 DOI: 10.1021/acs.jmedchem.6b01521
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 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.

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