[HTML][HTML] High-affinity activators of cystic fibrosis transmembrane conductance regulator (CFTR) chloride conductance identified by high-throughput screening
T Ma, L Vetrivel, H Yang, N Pedemonte… - Journal of Biological …, 2002 - ASBMB
Cystic fibrosis (CF) is caused by mutations in the CF transmembrane conductance regulator
(CFTR) protein that reduce cAMP-stimulated Cl− conductance in airway and other epithelia.
The purpose of this investigation was to identify new classes of potent CFTR activators. A
collection of 60,000 diverse drug-like compounds was screened at 10 μmtogether with a low
concentration of forskolin (0.5 μm) in Fisher rat thyroid epithelial cells co-expressing human
CFTR and a green fluorescent protein-based Cl− sensor. Primary screening yielded 57 …
(CFTR) protein that reduce cAMP-stimulated Cl− conductance in airway and other epithelia.
The purpose of this investigation was to identify new classes of potent CFTR activators. A
collection of 60,000 diverse drug-like compounds was screened at 10 μmtogether with a low
concentration of forskolin (0.5 μm) in Fisher rat thyroid epithelial cells co-expressing human
CFTR and a green fluorescent protein-based Cl− sensor. Primary screening yielded 57 …
