Discovery of novel potent ΔF 508‐CFTR correctors that target the nucleotide binding domain

…, EL Saussereau, P MelinHeschel… - EMBO Molecular …, 2013 - embopress.org
The deletion of Phe508 (ΔF508) in the first nucleotide binding domain (NBD1) of CFTR is
the most common mutation associated with cystic fibrosis. The ΔF508‐CFTR mutant is …

Identification of a novel water-soluble activator of wild-type and F508del CFTR: GPact-11a

…, B Boucherle, A Billet, P Melin-Heschel… - European …, 2010 - Eur Respiratory Soc
One of the major therapeutic strategy in cystic fibrosis aims at developing modulators of cystic
fibrosis transmembrane conductance regulator (CFTR) channels. We recently discovered …

[HTML][HTML] Stimulation of wild-type, F508del-and G551D-CFTR chloride channels by non-toxic modified pyrrolo [2, 3-b] pyrazine derivatives

…, A Billet, M Jollivet, P Melin-Heschel… - Frontiers in …, 2011 - frontiersin.org
Cystic fibrosis (CF) is a major inherited disorder involving abnormalities of fluid and
electrolyte transport in a number of different organs due to abnormal function of cystic fibrosis …

A functional tandem between transient receptor potential canonical channels 6 and calcium-dependent chloride channels in human epithelial cells

J Bertrand, L Dannhoffer, F Antigny, L Vachel… - European Journal of …, 2015 - Elsevier
… Values of P<0.05 were considered as statistically significant: *P<0.05; **… Cordi and P.
Bonnette for access to non-cystic fibrosis and cystic fibrosis human lung samples, respectively. This …

Overview of CFTR activators and their recent studies for dry eye disease: a review

J Wu, X Wang, Y Zhao, Y Hou, P Gong - RSC Medicinal Chemistry, 2023 - pubs.rsc.org
The cystic fibrosis transmembrane conductance regulator (CFTR) gets activated via the
cAMP signaling pathway and is present in various secretory epithelial cells, including …

Disease-modifying agents for the treatment of cystic fibrosis

BD Tait, JP Miller - Annual Reports in Medicinal Chemistry, 2014 - Elsevier
Cystic fibrosis is a genetic disease caused by mutations in the CFTR (cystic fibrosis transmembrane
conductance regulator) gene that affect transcription, folding, trafficking, degradation…

An expeditious access to 5-pyrimidinol derivatives from cyclic methylglyoxal diadducts, formation of argpyrimidines under physiological conditions and discovery of …

BL Renard, B Boucherle, B Maurin, MC Molina… - European journal of …, 2011 - Elsevier
In the study of previously reported modulators of CFTR chloride channels that are cyclic
methylglyoxal (MG) diadducts (CMGD) to aromatic α-aminoazaheterocycles, we optimized a …

Cystic fibrosis transmembrane regulator (CFTR) in human trophoblast BeWo cells and its relation to cell migration

GI Marino, BA Kotsias - Placenta, 2014 - Elsevier
Introduction ENaC and CFTR are coexpressed in epithelia and have positive or negative
functional interactions. In addition, ENaC and CFTR promote migration in placental …

REMD simulations reveal the dynamic profile and mechanism of action of deleterious, rescuing, and stabilizing perturbations to NBD1 from CFTR

M Zhenin, E Noy, H Senderowitz - Journal of chemical information …, 2015 - ACS Publications
Cystic Fibrosis (CF) is a lethal, genetic disease caused by mutations to the CFTR chloride
channel. The most common CF causing mutation is the deletion of F508 from the first …

A new 9-alkyladenine-cyclic methylglyoxal diadduct activates wt-and F508del-cystic fibrosis transmembrane conductance regulator (CFTR) in vitro and in vivo

B Boucherle, J Bertrand, B Maurin, BL Renard… - European Journal of …, 2014 - Elsevier
Cystic fibrosis transmembrane conductance regulator (CFTR) is the main chloride channel
present in the apical membrane of epithelial cells and the F508 deletion (F508del-CFTR) in …