Literature DB >> 22281185

Fluorinated ΔF508-CFTR correctors and potentiators for PET imaging.

Holly R Davison1, Danielle M Solano, Puay-Wah Phuan, A S Verkman, Mark J Kurth.   

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.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 22281185      PMCID: PMC3274619          DOI: 10.1016/j.bmcl.2011.12.128

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  26 in total

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Authors:  Philip W Miller; Nicholas J Long; Ramon Vilar; Antony D Gee
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Review 2.  Current and emerging imaging in relation to drug discovery in airways disease.

Authors:  Gregory G King
Journal:  Pulm Pharmacol Ther       Date:  2011-07-23       Impact factor: 3.410

3.  Functional fluorescently labeled bithiazole ΔF508-CFTR corrector imaged in whole body slices in mice.

Authors:  Holly R Davison; Stephanie Taylor; Chris Drake; Puay-Wah Phuan; Nico Derichs; Chenjuan Yao; Ella F Jones; Julie Sutcliffe; A S Verkman; Mark J Kurth
Journal:  Bioconjug Chem       Date:  2011-11-18       Impact factor: 4.774

Review 4.  From tumor biology to clinical Pet: a review of positron emission tomography (PET) in oncology.

Authors:  K Kubota
Journal:  Ann Nucl Med       Date:  2001-12       Impact factor: 2.668

5.  Design and synthesis of a hybrid potentiator-corrector agonist of the cystic fibrosis mutant protein DeltaF508-CFTR.

Authors:  Aaron D Mills; Choong Yoo; Jeffrey D Butler; Baoxue Yang; A S Verkman; Mark J Kurth
Journal:  Bioorg Med Chem Lett       Date:  2009-11-13       Impact factor: 2.823

6.  Potent s-cis-locked bithiazole correctors of DeltaF508 cystic fibrosis transmembrane conductance regulator cellular processing for cystic fibrosis therapy.

Authors:  Gui Jun Yu; Choong L Yoo; Baoxue Yang; Michael W Lodewyk; Liping Meng; Tamer T El-Idreesy; James C Fettinger; Dean J Tantillo; A S Verkman; Mark J Kurth
Journal:  J Med Chem       Date:  2008-09-13       Impact factor: 7.446

7.  Processing of mutant cystic fibrosis transmembrane conductance regulator is temperature-sensitive.

Authors:  G M Denning; M P Anderson; J F Amara; J Marshall; A E Smith; M J Welsh
Journal:  Nature       Date:  1992-08-27       Impact factor: 49.962

8.  Long term prognosis of patients with cystic fibrosis in relation to early detection by neonatal screening and treatment in a cystic fibrosis centre.

Authors:  J E Dankert-Roelse; G J te Meerman
Journal:  Thorax       Date:  1995-07       Impact factor: 9.139

9.  Synthesis of aryl azides and vinyl azides via proline-promoted CuI-catalyzed coupling reactions.

Authors:  Wei Zhu; Dawei Ma
Journal:  Chem Commun (Camb)       Date:  2004-03-05       Impact factor: 6.222

10.  Phenylglycine and sulfonamide correctors of defective delta F508 and G551D cystic fibrosis transmembrane conductance regulator chloride-channel gating.

Authors:  Nicoletta Pedemonte; N D Sonawane; Alessandro Taddei; Jie Hu; Olga Zegarra-Moran; Yat Fan Suen; Lori I Robins; Christopher W Dicus; Dan Willenbring; Michael H Nantz; Mark J Kurth; Luis J V Galietta; A S Verkman
Journal:  Mol Pharmacol       Date:  2005-02-18       Impact factor: 4.436

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  1 in total

Review 1.  An Overview of the Synthesis and Antimicrobial, Antiprotozoal, and Antitumor Activity of Thiazole and Bisthiazole Derivatives.

Authors:  Anca-Maria Borcea; Ioana Ionuț; Ovidiu Crișan; Ovidiu Oniga
Journal:  Molecules       Date:  2021-01-25       Impact factor: 4.411

  1 in total

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