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    ISSN : 2328-9791
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Novel aminoarylthiazole derivatives as correctors of the chloride transport defect in cystic fibrosis: computer assisted drug design, synthesis and biological evaluation
     
 
Author(s) : Liessi N, Cichero E, Pesce E, D’Ursi P, Salis A, Pedemonte N, Damonte G, Galietta LJV, Fossa P, Millo E
Address : University of Genoa, Istituto Giannina Gaslini, Institute for Biomedical Technologies e National Research Council, Italy.
Multiple Institutions in Collaboration
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Background. CF is caused by mutations that abolish the function of CFTR, a protein that is needed to transport chloride and bicarbonate across cell membrane in the epithelial cells. The most frequent mutation, F508del requires a specific pharmacological treatment. Such defects can be addressed with small molecules, known as correctors and potentiators. In previous studies, we identified a class of compounds called aminoarylthiazoles (AATs) that potentially correct the CF basic defect.

Hypothesis and objectives. The main objective of our project is to identify new AATs which could be efficiently able to correct the CFTR protein defect caused by F508del. By using an integrated approach (bioinformatics, chemical synthesis, and functional assays) we will aim at developing drug- like compounds with improved activity on mutant CFTR.

 
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