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Fluorinated ?F508-CFTR correctors and potentiators for PET imaging.


ABSTRACT: (19)F-modified bithiazole correctors and phenylglycine potentiators of the ?F508-CFTR chloride channel were synthesized and their function assayed in cells expressing human ?F508-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 ?F508-CFTR corrector and potentiator potencies of the fluorinated analogs were comparable to or better than those of the original compounds.

SUBMITTER: Davison HR 

PROVIDER: S-EPMC3274619 | biostudies-literature | 2012 Feb

REPOSITORIES: biostudies-literature

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Fluorinated ΔF508-CFTR correctors and potentiators for PET imaging.

Davison Holly R HR   Solano Danielle M DM   Phuan Puay-Wah PW   Verkman A S AS   Kurth Mark J MJ  

Bioorganic & medicinal chemistry letters 20120103 4


(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  ...[more]

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