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 › peer-review

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 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

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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AU - Davison, Holly R.

AU - Solano, Danielle M.

AU - Phuan, Puay Wah

AU - Verkman, A. S.

AU - Kurth, Mark J.

PY - 2012/2/15

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AB - 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.

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KW - PET

KW - Potentiator

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Fluorinated DF508-CFTR correctors and potentiators for PET imaging

Abstract

Keywords

ASJC Scopus subject areas

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