Fluorinated DF508-CFTR correctors and potentiators for PET imaging

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

doi:10.1016/j.bmcl.2011.12.128

Fluorinated DF508-CFTR correctors and potentiators for PET imaging

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

Chemistry

Research output: Contribution to journal › Article

2 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 language	English (US)
Pages (from-to)	1602-1605
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	22
Issue number	4
DOIs	https://doi.org/10.1016/j.bmcl.2011.12.128
State	Published - Feb 15 2012

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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)

Cite this

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

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10.1016/j.bmcl.2011.12.128