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期刊论文
High-affinity Activators of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Chloride Conductance Identified by High-throughput Screening*
THE JOURNAL OF BIOLOGICAL CHEMISTRY Vol. 277, No.40, Issue of October 4, pp. 37235-37241, 2002，-0001，（）：
and were CFTR-selective, reversible, and nontoxic. Several compounds, the most potent being a trifluoromethylphenylbenzamine, activated the CF-causing mutant G551D, but with much weaker affinity (Kd>10M). When added for 10min, none of the compounds activated Phe508-CFTR in transfected cells grown at 37℃ (with Phe508-CFTR trapped in the endoplasmic reticulum). However, after correction of trafficking by 48h of growth at 27℃, tetrahydrocarbazol and N-phenyltriazine derivatives strongly stimulated Cl conductance with Kd<1M. The new activators identified here may be useful in defining molecular mechanisms of CFTR activation and as lead compounds in CF drug development.
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