Structure–activity relationships of cyanoquinolines with corrector–potentiator activity in δF508 cystic fibrosis transmembrane conductance regulator protein

…, MW Lodewyk, DJ Tantillo, AS Verkman…

文献索引：Knapp, John M.; Wood, Alex B.; Phuan, Puay-Wah; Lodewyk, Michael W.; Tantillo, Dean J.; Verkman; Kurth, Mark J. Journal of Medicinal Chemistry, 2012 , vol. 55, # 3 p. 1242 - 1251

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被引用次数: 15

摘要

Cystic fibrosis (CF) is caused by mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel. The most common CF-causing mutation, ΔF508-CFTR, produces CFTR loss-of-function by impairing its cellular targeting to the plasma membrane and its chloride channel gating. We recently identified cyanoquinolines with both corrector (“Co”, normalizing ΔF508-CFTR targeting) and potentiator (“Po”, normalizing ΔF508-CFTR ...