title: Fluorinated ΔF508-CFTR correctors and potentiators for PET imaging.
abstract: (19)F-modified bithiazole correctors and phenylglycine potentiators of the ΔF508-CFTR chloride channel were synthesized and their function assayed in cells expressing human ΔF508-CFTR and a halide-sensitive fluorescent protein. Fluorine was incorporated into each scaffold using prosthetic groups for future biodistribution imaging studies using positron emission tomography (PET). The ΔF508-CFTR corrector and potentiator potencies of the fluorinated analogs were comparable to or better than those of the original compounds.
authors.affiliation: Department of Chemistry, University of California, Davis, Davis, CA 95616, United States.
authors.forename: Holly R
authors.initials: HR
authors.lastname: Davison
authors.forename: Danielle M
authors.initials: DM
authors.lastname: Solano
authors.forename: Puay-Wah
authors.initials: PW
authors.lastname: Phuan
authors.forename: A S
authors.initials: AS
authors.lastname: Verkman
authors.forename: Mark J
authors.initials: MJ
authors.lastname: Kurth
mesh_terms: D019005:Cystic Fibrosis Transmembrane Conductance Regulator / Q000737:chemistry*; D005462:Fluorine Radioisotopes; D006801:Humans; D015394:Molecular Structure; D049268:Positron-Emission Tomography / Q000379:methods*
chemical_list: D005462:Fluorine Radioisotopes; C093349:cystic fibrosis transmembrane conductance regulator delta F508; D019005:Cystic Fibrosis Transmembrane Conductance Regulator