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 …

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 …

Orkambi® and amplifier co‐therapy improves function from a rare CFTR mutation in gene‐edited cells and patient tissue

SV Molinski, S Ahmadi, W Ip, H Ouyang… - EMBO molecular …, 2017 - embopress.org
The combination therapy of lumacaftor and ivacaftor (Orkambi®) is approved for patients
bearing the major cystic fibrosis (CF) mutation: ΔF508. It has been predicted that Orkambi® …

Identifying the molecular target sites for CFTR potentiators GLPG1837 and VX-770

HI Yeh, L Qiu, Y Sohma, K Conrath, X Zou… - Journal of General …, 2019 - rupress.org
The past two decades have witnessed major breakthroughs in developing compounds that
target the chloride channel CFTR for the treatment of patients with cystic fibrosis. However …

[HTML][HTML] One size does not fit all: the past, present and future of cystic fibrosis causal therapies

MM Ensinck, MS Carlon - Cells, 2022 - mdpi.com
Cystic fibrosis (CF) is the most common monogenic disorder, caused by mutations in the CF
transmembrane conductance regulator (CFTR) gene. Over the last 30 years, tremendous …

Identification of binding sites for ivacaftor on the cystic fibrosis transmembrane conductance regulator

O Laselva, Z Qureshi, ZW Zeng, EV Petrotchenko… - Iscience, 2021 - cell.com
Summary Ivacaftor (VX-770) was the first cystic fibrosis transmembrane conductance
regulator (CFTR) modulatory drug approved for the treatment of patients with cystic fibrosis …

A common mechanism for CFTR potentiators

HI Yeh, Y Sohma, K Conrath, TC Hwang - Journal of General …, 2017 - rupress.org
Cystic fibrosis (CF) is a channelopathy caused by loss-of-function mutations of the cystic
fibrosis transmembrane conductance regulator (CFTR) gene, which encodes a …

Timing of CFTR pore opening and structure of its transition state

B Sorum, D Czégé, L Csanády - Cell, 2015 - cell.com
In CFTR, the chloride ion channel mutated in cystic fibrosis (CF) patients, pore opening is
coupled to ATP-binding-induced dimerization of two cytosolic nucleotide binding domains …

The molecular evolution of function in the CFTR chloride channel

DT Infield, KM Strickland, A Gaggar… - Journal of General …, 2021 - rupress.org
The ATP-binding cassette (ABC) transporter superfamily includes many proteins of clinical
relevance, with genes expressed in all domains of life. Although most members use the …

Structure basis of CFTR folding, function and pharmacology

TC Hwang, I Braakman, P van der Sluijs… - Journal of Cystic …, 2023 - Elsevier
The root cause of cystic fibrosis (CF), the most common life-shortening genetic disease in
the Caucasian population, is the loss of function of the CFTR protein, which serves as a …