Article
Macrocycle-stabilization of its interaction with 14-3-3 increases plasma membrane localization and activity of CFTR.
Nature communications - 23 Jun 2022
Stevers Loes M, Wolter Madita, Carlile Graeme W, Macdonald Dwight, Richard Luc, Gielkens Frank, Hanrahan John W, Thomas David Y, Chakka Sai Kumar, Peterson Mark L, Thomas Helmut, Brunsveld Luc, Ottmann Christian
Abstract excerpt
Impaired activity of the chloride channel CFTR is the cause of cystic fibrosis. 14-3-3 proteins have been shown to stabilize CFTR and increase its biogenesis and activity. Here, we report the identification and mechanism of action of a macrocycle stabilizing the 14-3-3/CFTR complex. This molecule rescues plasma membrane localization and chloride transport of F508del-CFTR and works additively with the CFTR...
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