Potentiation of ΔF508- and G551D-CFTR-Mediated Cl- Current by Novel Hydroxypyrazolines

The most common mutation of CFTR, affecting approximately 90% of CF patients, is a deletion of phenylalanine at position 508 (F508del, ΔF508). Misfolding of ΔF508-CFTR impairs both its trafficking to the plasma membrane and its chloride channel activity. To identify small molecules that can restore...

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Veröffentlicht in:	PloS one 2016-02, Vol.11 (2), p.e0149131-e0149131
Hauptverfasser:	Park, Jinhong, Khloya, Poonam, Seo, Yohan, Kumar, Satish, Lee, Ho K, Jeon, Dong-Kyu, Jo, Sungwoo, Sharma, Pawan K, Namkung, Wan
Format:	Artikel
Sprache:	eng
Schlagworte:	Aminopyridines - therapeutic use Animals Bacterial Proteins - chemistry Benzodioxoles - therapeutic use Biology and Life Sciences Cell Line Cell Line, Tumor Cell Membrane - metabolism Cell Proliferation Channel gating Chemical synthesis Chloride Chloride conductance Chlorides Chlorides - chemistry Clinical trials Cyclic AMP - metabolism Cystic fibrosis Cystic Fibrosis - drug therapy Cystic Fibrosis - genetics Cystic Fibrosis Transmembrane Conductance Regulator - genetics Cytotoxicity Defects Epithelial Cells - cytology Gene Deletion Genistein Genistein - chemistry Humans Kinases Luminescent Proteins - chemistry Medicine and Health Sciences Membrane trafficking Mutation Nose - physiology Patch-Clamp Techniques Pharmaceutical sciences Pharmacy Phenylalanine Phenylalanine - genetics Physical Sciences Plasma Potentiation Proteins Pyrazoles - therapeutic use Rats Research and analysis methods Resistance Structure-Activity Relationship Sulfonamides - therapeutic use Toxicity
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