Literature DB >> 18394886

4'-Methyl-4,5'-bithiazole-based correctors of defective delta F508-CFTR cellular processing.

Choong Leol Yoo1, Gui Jun Yu, Baoxue Yang, Lori I Robins, A S Verkman, Mark J Kurth.   

Abstract

The synthesis and Delta F508-CFTR corrector activity of a 148-member methylbithiazole-based library are reported. Synthetic routes were devised and optimized to generate methylbithiazole analogs in four steps. Corrector potency and efficacy were assayed using epithelial cells expressing human Delta F508-CFTR. These structure-activity data establish that the bithiazole substructure plays a critical function; eight novel methylbithiazole correctors were identified with low micromolar potencies.

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Year:  2008        PMID： 18394886      PMCID： PMC3166558          DOI： 10.1016/j.bmcl.2008.03.037

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


  13 in total

Review 1.  Cystic fibrosis transmembrane conductance regulator. Structure and function of an epithelial chloride channel.

Authors:  M H Akabas
Journal:  J Biol Chem       Date:  2000-02-11       Impact factor: 5.157

2.  Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin-induced intestinal fluid secretion.

Authors:  Tonghui Ma; Jay R Thiagarajah; Hong Yang; Nitin D Sonawane; Chiara Folli; Luis J V Galietta; A S Verkman
Journal:  J Clin Invest       Date:  2002-12       Impact factor: 14.808

3.  Genistein potentiates wild-type and delta F508-CFTR channel activity.

Authors:  T C Hwang; F Wang; I C Yang; W W Reenstra
Journal:  Am J Physiol       Date:  1997-09

4.  Chloride conductance expressed by delta F508 and other mutant CFTRs in Xenopus oocytes.

Authors:  M L Drumm; D J Wilkinson; L S Smit; R T Worrell; T V Strong; R A Frizzell; D C Dawson; F S Collins
Journal:  Science       Date:  1991-12-20       Impact factor: 47.728

Review 5.  Molecular pharmacology of the CFTR Cl- channel.

Authors:  T C Hwang; D N Sheppard
Journal:  Trends Pharmacol Sci       Date:  1999-11       Impact factor: 14.819

Review 6.  Cystic fibrosis: a worldwide analysis of CFTR mutations--correlation with incidence data and application to screening.

Authors:  Joseph L Bobadilla; Milan Macek; Jason P Fine; Philip M Farrell
Journal:  Hum Mutat       Date:  2002-06       Impact factor: 4.878

7.  Green fluorescent protein-based halide indicators with improved chloride and iodide affinities.

Authors:  L J Galietta; P M Haggie; A S Verkman
Journal:  FEBS Lett       Date:  2001-06-22       Impact factor: 4.124

Review 8.  Structure and function of the CFTR chloride channel.

Authors:  D N Sheppard; M J Welsh
Journal:  Physiol Rev       Date:  1999-01       Impact factor: 37.312

9.  Small-molecule correctors of defective DeltaF508-CFTR cellular processing identified by high-throughput screening.

Authors:  Nicoletta Pedemonte; Gergely L Lukacs; Kai Du; Emanuela Caci; Olga Zegarra-Moran; Luis J V Galietta; A S Verkman
Journal:  J Clin Invest       Date:  2005-08-25       Impact factor: 14.808

10.  COOH-terminal truncations promote proteasome-dependent degradation of mature cystic fibrosis transmembrane conductance regulator from post-Golgi compartments.

Authors:  M Benharouga; M Haardt; N Kartner; G L Lukacs
Journal:  J Cell Biol       Date:  2001-05-28       Impact factor: 10.539
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  19 in total

1.  Pyrazolylthiazole as DeltaF508-cystic fibrosis transmembrane conductance regulator correctors with improved hydrophilicity compared to bithiazoles.

Authors:  Long Ye; John M Knapp; Panjamaporn Sangwung; James C Fettinger; A S Verkman; Mark J Kurth
Journal:  J Med Chem       Date:  2010-05-13       Impact factor: 7.446

2.  Fluorinated ΔF508-CFTR correctors and potentiators for PET imaging.

Authors:  Holly R Davison; Danielle M Solano; Puay-Wah Phuan; A S Verkman; Mark J Kurth
Journal:  Bioorg Med Chem Lett       Date:  2012-01-03       Impact factor: 2.823

3.  Enhancing the Potency of F508del Correction: A Multi-Layer Combinational Approach to Drug Discovery for Cystic Fibrosis.

Authors:  Emily F Kirby; Ashley S Heard; X Robert Wang
Journal:  J Pharmacol Clin Toxicol       Date:  2013-08-28

4.  ΔF508-CFTR correctors: synthesis and evaluation of thiazole-tethered imidazolones, oxazoles, oxadiazoles, and thiadiazoles.

Authors:  Long Ye; Bao Hu; Faris El-Badri; Brandi M Hudson; Puay-Wah Phuan; A S Verkman; Dean J Tantillo; Mark J Kurth
Journal:  Bioorg Med Chem Lett       Date:  2014-10-02       Impact factor: 2.823

Review 5.  CFTR pharmacology.

Authors:  Olga Zegarra-Moran; Luis J V Galietta
Journal:  Cell Mol Life Sci       Date:  2016-10-04       Impact factor: 9.261

6.  Structure-activity relationships of cyanoquinolines with corrector-potentiator activity in ΔF508 cystic fibrosis transmembrane conductance regulator protein.

Authors:  John M Knapp; Alex B Wood; Puay-Wah Phuan; Michael W Lodewyk; Dean J Tantillo; A S Verkman; Mark J Kurth
Journal:  J Med Chem       Date:  2012-01-23       Impact factor: 7.446

7.  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

8.  Click-based synthesis of triazolobithiazole ΔF508-CFTR correctors for cystic fibrosis.

Authors:  Michael B Donald; Kevin X Rodriguez; Hannah Shay; Puay-Wah Phuan; A S Verkman; Mark J Kurth
Journal:  Bioorg Med Chem       Date:  2012-07-06       Impact factor: 3.641

9.  Isoxazolopyrimidines as Novel ΔF508-CFTR Correctors.

Authors:  Gui Jun Yu; Baoxue Yang; A S Verkman; Mark J Kurth
Journal:  Synlett       Date:  2010-04-01       Impact factor: 2.454

10.  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
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