Fluorinated ΔF508-CFTR correctors and potentiators for PET imaging

Bioorg Med Chem Lett. 2012 Feb 15;22(4):1602-5. doi: 10.1016/j.bmcl.2011.12.128. Epub 2012 Jan 3.

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.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Cystic Fibrosis Transmembrane Conductance Regulator / chemistry*
  • Fluorine Radioisotopes*
  • Humans
  • Molecular Structure
  • Positron-Emission Tomography / methods*

Substances

  • Fluorine Radioisotopes
  • cystic fibrosis transmembrane conductance regulator delta F508
  • Cystic Fibrosis Transmembrane Conductance Regulator