[HTML][HTML] Novel CFTR Chloride Channel Activators Identified by Screening of Combinatorial Libraries Based on Flavone and Benzoquinolizinium Lead Compounds …
LJV Galietta, MF Springsteel, M Eda… - Journal of Biological …, 2001 - ASBMB
The flavonoid genistein and the benzo [c] quinolizinium MPB-07 have been shown to
activate the cystic fibrosis transmembrane conductance regulator (CFTR), the protein that is
defective in cystic fibrosis. Lead-based combinatorial and parallel synthesis yielded 223
flavonoid, quinolizinium, and related heterocyclic compounds. The compounds were
screened for their ability to activate CFTR at 50 μmconcentration by measurement of the
kinetics of iodide influx in Fisher rat thyroid cells expressing wild-type or G551D CFTR …
activate the cystic fibrosis transmembrane conductance regulator (CFTR), the protein that is
defective in cystic fibrosis. Lead-based combinatorial and parallel synthesis yielded 223
flavonoid, quinolizinium, and related heterocyclic compounds. The compounds were
screened for their ability to activate CFTR at 50 μmconcentration by measurement of the
kinetics of iodide influx in Fisher rat thyroid cells expressing wild-type or G551D CFTR …