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

4 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)

Access to Document

10.1016/j.bmcl.2011.12.128

Cite this

@article{9902fd6887dc413babd44638d63144a7,

title = "Fluorinated DF508-CFTR correctors and potentiators for PET imaging",

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.",

keywords = "Corrector, Cystic fibrosis, DF508-CFTR, PET, Potentiator",

author = "Davison, {Holly R.} and Solano, {Danielle M.} and Phuan, {Puay Wah} and Verkman, {A. S.} and Kurth, {Mark J.}",

year = "2012",

month = feb,

day = "15",

doi = "10.1016/j.bmcl.2011.12.128",

language = "English (US)",

volume = "22",

pages = "1602--1605",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Limited",

number = "4",

}

TY - JOUR

T1 - Fluorinated DF508-CFTR correctors and potentiators for PET imaging

AU - Davison, Holly R.

AU - Solano, Danielle M.

AU - Phuan, Puay Wah

AU - Verkman, A. S.

AU - Kurth, Mark J.

PY - 2012/2/15

Y1 - 2012/2/15

N2 - 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.

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.

KW - Corrector

KW - Cystic fibrosis

KW - DF508-CFTR

KW - PET

KW - Potentiator

UR - http://www.scopus.com/inward/record.url?scp=84856647972&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84856647972&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2011.12.128

DO - 10.1016/j.bmcl.2011.12.128

M3 - Article

C2 - 22281185

AN - SCOPUS:84856647972

VL - 22

SP - 1602

EP - 1605

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

IS - 4

ER -

Fluorinated DF508-CFTR correctors and potentiators for PET imaging

Abstract

Keywords

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this