New insights into structure and function of bis-phosphinic acid derivatives and implications for CFTR modulation.

doi:10.1038/s41598-021-83240-x

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Article

New insights into structure and function of bis-phosphinic acid derivatives and implications for CFTR modulation.

Scientific reports - 25 Mar 2021

Bitam Sara, Elbahnsi Ahmad, Creste Geordie, Pranke Iwona, Chevalier Benoit, Berhal Farouk, Hoffmann Brice, Servel Nathalie, Baatalah Nesrine, Tondelier Danielle, Hatton Aurelie, Moquereau Christelle, Faria Da Cunha Mélanie, Pastor Alexandra, Lepissier Agathe, Hinzpeter Alexandre, Mornon Jean-Paul, Prestat Guillaume, Edelman Aleksander, Callebaut Isabelle, Gravier-Pelletier Christine, Sermet-Gaudelus Isabelle

Abstract excerpt

C407 is a compound that corrects the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) protein carrying the p.Phe508del (F508del) mutation. We investigated the corrector effect of c407 and its derivatives on F508del-CFTR protein. Molecular docking and dynamics simulations combined with site-directed mutagenesis suggested that c407 stabilizes the F508del-Nucleotide Binding Domain 1 (NBD1) during the...

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PMID: 33767236
DOI: 10.1038/s41598-021-83240-x
PMCID: PMC7994384

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