Article
Synthesis and biological evaluation of novel thiazole- VX-809 hybrid derivatives as F508del correctors by QSAR-based filtering tools.
European journal of medicinal chemistry - 20 Jan 2018
Liessi Nara, Cichero Elena, Pesce Emanuela, Arkel Maria, Salis Annalisa, Tomati Valeria, Paccagnella Matteo, Damonte Gianluca, Tasso Bruno, Galietta Luis J V, Pedemonte Nicoletta, Fossa Paola, Millo Enrico
Abstract excerpt
The most common CF mutation, F508del, impairs the processing and gating of CFTR protein. This deletion results in the improper folding of the protein and its degradation before it reaches the plasma membrane of epithelial cells. Present correctors, like VX809 only induce a partial rescue of the mutant protein. Our previous studies reported a class of compounds, called aminoarylthiazoles (AATs), featuring an...
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