Add to ORKGThe most common mutation causing cystic fibrosis (CF) is deletion of phenylalanine residue 508 in the cystic fibrosis transmembrane regulator conductance (CFTR) protein. Small molecules that are able to correct the misfolding of defective ΔF508-CFTR have considerable promise for therapy. Reported here are the design, preparation, and evaluation of five more hydrophilic bisazole analogs of previously identified bithiazole CF corrector 1. Interestingly, bisazole ΔF508-CFTR corrector activity was not increased by incorporation of more H-bond acceptors (O or N), but correlated best with the overall bisazole molecular geometry. The structure activity data, together with molecular modeling, suggested that active bisazole correctors adopt a U-shap...
Better correctors are needed to repair cystic fibrosis transmembrane conductance regulator (CFTR) pr...
The phenylhydrazone RDR-1 is endowed with moderate activity as F508del-CFTR corrector; nevertheless,...
Cystic fibrosis (CF) is the autosomal recessive disorder most recurrent in Caucasian populations. It...
The most common mutation causing cystic fibrosis (CF) is deletion of phenylalanine residue 508 in th...
Cystic fibrosis (CF) is a genetic disease caused by mutations that impair the function of the CFTR c...
none5noCystic fibrosis is a genetic disease caused by loss-of-function mutations in the cystic fibro...
The cystic fibrosis transmembrane conductance regulator (CFTR) is a chloride channel present in the m...
Conformationally constrained bithiazoles were previously found to have improved efficacy over noncon...
The F508del mutation impairs the trafficking of CFTR from endoplasmic reticulum to plasma membrane a...
Small-molecule therapies that restore defects in cystic fibrosis transmembrane conductance regulator...
The most common cause of cystic fibrosis (CF) is deletion of phenylalanine 508 (DeltaF508) in the CF...
Cystic fibrosis (CF) is caused by loss-of-function mutations in the CF transmembrane conductance reg...
Cystic fibrosis (CF) is caused by loss-of-function mutations in the CF transmembrane conductance reg...
Cystic fibrosis (CF) is a lethal genetic disease caused by mutations of the gene encoding the cystic...
The lack of phenylalanine 508 (ΔF508 mutation) in the cystic fibrosis (CF) transmembrane conductance...
Better correctors are needed to repair cystic fibrosis transmembrane conductance regulator (CFTR) pr...
The phenylhydrazone RDR-1 is endowed with moderate activity as F508del-CFTR corrector; nevertheless,...
Cystic fibrosis (CF) is the autosomal recessive disorder most recurrent in Caucasian populations. It...
The most common mutation causing cystic fibrosis (CF) is deletion of phenylalanine residue 508 in th...
Cystic fibrosis (CF) is a genetic disease caused by mutations that impair the function of the CFTR c...
none5noCystic fibrosis is a genetic disease caused by loss-of-function mutations in the cystic fibro...
The cystic fibrosis transmembrane conductance regulator (CFTR) is a chloride channel present in the m...
Conformationally constrained bithiazoles were previously found to have improved efficacy over noncon...
The F508del mutation impairs the trafficking of CFTR from endoplasmic reticulum to plasma membrane a...
Small-molecule therapies that restore defects in cystic fibrosis transmembrane conductance regulator...
The most common cause of cystic fibrosis (CF) is deletion of phenylalanine 508 (DeltaF508) in the CF...
Cystic fibrosis (CF) is caused by loss-of-function mutations in the CF transmembrane conductance reg...
Cystic fibrosis (CF) is caused by loss-of-function mutations in the CF transmembrane conductance reg...
Cystic fibrosis (CF) is a lethal genetic disease caused by mutations of the gene encoding the cystic...
The lack of phenylalanine 508 (ΔF508 mutation) in the cystic fibrosis (CF) transmembrane conductance...
Better correctors are needed to repair cystic fibrosis transmembrane conductance regulator (CFTR) pr...
The phenylhydrazone RDR-1 is endowed with moderate activity as F508del-CFTR corrector; nevertheless,...
Cystic fibrosis (CF) is the autosomal recessive disorder most recurrent in Caucasian populations. It...