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Article

Constrained bithiazoles: small molecule correctors of defective ΔF508-CFTR protein trafficking.

Journal of medicinal chemistry - 14 Aug 2014

Coffman Keith C, Nguyen Huy H, Phuan Puay-Wah, Hudson Brandi M, Yu Gui J, Bagdasarian Alex L, Montgomery Deanna, Lodewyk Michael W, Yang Baoxue, Yoo Choong L, Verkman A S, Tantillo Dean J, Kurth Mark J

Abstract excerpt

Conformationally constrained bithiazoles were previously found to have improved efficacy over nonconstrained bithiazoles for correction of defective cellular processing of the ΔF508 mutant cystic fibrosis transmembrane conductance regulator (CFTR) protein. In this study, two sets of constrained bithiazoles were designed, synthesized, and tested in vitro using ΔF508-CFTR expressing epithelial cells. The SAR data...

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Share to Cystic Fibrosis Transmembrane Conductance Regulator

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Source

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Identifiers

PMID: 25061695
DOI: 10.1021/jm5007885
PMCID: PMC4136667

Genes

CFTR

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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