Article
Targeting different binding sites in the CFTR structures allows to synergistically potentiate channel activity.
European journal of medicinal chemistry - 15 Mar 2020
Froux Lionel, Elbahnsi Ahmad, Boucherle Benjamin, Billet Arnaud, Baatallah Nesrine, Hoffmann Brice, Alliot Julien, Zelli Renaud, Zeinyeh Wael, Haudecoeur Romain, Chevalier Benoit, Fortuné Antoine, Mirval Sandra, Simard Christophe, Lehn Pierre, Mornon Jean-Paul, Hinzpeter Alexandre, Becq Frédéric, Callebaut Isabelle, Décout Jean-Luc
Abstract excerpt
Recent evidence shows that combination of correctors and potentiators, such as the drug ivacaftor (VX-770), can significantly restore the functional expression of mutated Cystic Fibrosis Transmembrane conductance Regulator (CFTR), an anion channel which is mutated in cystic fibrosis (CF). The success of these combinatorial therapies highlights the necessity of identifying a broad panel of specific binding mode...
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