Fluorinated DF508-CFTR correctors and potentiators for PET imaging

Holly R. Davison, Danielle M. Solano, Puay Wah Phuan, A. S. Verkman, Mark J. Kurth

Research output: Contribution to journalArticle

3 Scopus citations

Abstract

19F-modified bithiazole correctors and phenylglycine potentiators of the DF508-CFTR chloride channel were synthesized and their function assayed in cells expressing human DF508-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 DF508-CFTR corrector and potentiator potencies of the fluorinated analogs were comparable to or better than those of the original compounds.

Original languageEnglish (US)
Pages (from-to)1602-1605
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume22
Issue number4
DOIs
StatePublished - Feb 15 2012

Keywords

  • Corrector
  • Cystic fibrosis
  • DF508-CFTR
  • PET
  • Potentiator

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry
  • Medicine(all)

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    Davison, H. R., Solano, D. M., Phuan, P. W., Verkman, A. S., & Kurth, M. J. (2012). Fluorinated DF508-CFTR correctors and potentiators for PET imaging. Bioorganic and Medicinal Chemistry Letters, 22(4), 1602-1605. https://doi.org/10.1016/j.bmcl.2011.12.128