From CFTR biology toward combinatorial pharmacotherapy: expanded classification of cystic fibrosis mutations

G Veit, RG Avramescu, AN Chiang… - Molecular biology of …, 2016 - Am Soc Cell Biol
More than 2000 mutations in the cystic fibrosis transmembrane conductance regulator
(CFTR) have been described that confer a range of molecular cell biological and functional …

Structure, gating, and regulation of the CFTR anion channel

L Csanády, P Vergani, DC Gadsby - Physiological reviews, 2019 - journals.physiology.org
The cystic fibrosis transmembrane conductance regulator (CFTR) belongs to the ATP
binding cassette (ABC) transporter superfamily but functions as an anion channel crucial for …

[HTML][HTML] CFTR function, pathology and pharmacology at single-molecule resolution

J Levring, DS Terry, Z Kilic, G Fitzgerald, SC Blanchard… - Nature, 2023 - nature.com
The cystic fibrosis transmembrane conductance regulator (CFTR) is an anion channel that
regulates salt and fluid homeostasis across epithelial membranes. Alterations in CFTR …

[HTML][HTML] Atomic structure of the cystic fibrosis transmembrane conductance regulator

Z Zhang, J Chen - Cell, 2016 - cell.com
The cystic fibrosis transmembrane conductance regulator (CFTR) is an anion channel
evolved from the ATP-binding cassette (ABC) transporter family. In this study, we determined …

Potentiator ivacaftor abrogates pharmacological correction of ΔF508 CFTR in cystic fibrosis

DM Cholon, NL Quinney, ML Fulcher… - Science translational …, 2014 - science.org
Cystic fibrosis (CF) is caused by mutations in the CF transmembrane conductance regulator
(CFTR). Newly developed “correctors” such as lumacaftor (VX-809) that improve CFTR …

Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Potentiator VX-770 (Ivacaftor) Opens the Defective Channel Gate of Mutant CFTR in a …

PDW Eckford, C Li, M Ramjeesingh, CE Bear - Journal of Biological …, 2012 - ASBMB
The cystic fibrosis transmembrane conductance regulator (CFTR) acts as a channel on the
apical membrane of epithelia. Disease-causing mutations in the cystic fibrosis gene can …

Conformational changes of CFTR upon phosphorylation and ATP binding

Z Zhang, F Liu, J Chen - Cell, 2017 - cell.com
The cystic fibrosis transmembrane conductance regulator (CFTR) is an anion channel
evolved from an ATP-binding cassette transporter. CFTR channel gating is strictly coupled to …

Vx-770 potentiates CFTR function by promoting decoupling between the gating cycle and ATP hydrolysis cycle

KY Jih, TC Hwang - … of the National Academy of Sciences, 2013 - National Acad Sciences
Vx-770 (Ivacaftor), a Food and Drug Administration (FDA)-approved drug for clinical
application to patients with cystic fibrosis (CF), shifts the paradigm from conventional …

Structural mechanisms of CFTR function and dysfunction

TC Hwang, JT Yeh, J Zhang, YC Yu, HI Yeh… - Journal of General …, 2018 - rupress.org
Cystic fibrosis (CF) transmembrane conductance regulator (CFTR) chloride channel plays a
critical role in regulating transepithelial movement of water and electrolyte in exocrine …

[HTML][HTML] Residual function of cystic fibrosis mutants predicts response to small molecule CFTR modulators

ST Han, A Rab, MJ Pellicore, EF Davis, AF McCague… - JCI insight, 2018 - ncbi.nlm.nih.gov
Abstract Treatment of individuals with cystic fibrosis (CF) has been transformed by small
molecule therapies that target select pathogenic variants in the CF transmembrane …