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Article

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

Bioorganic & medicinal chemistry letters - 1 Jan 2010

Mills Aaron D, Yoo Choong, Butler Jeffrey D, Yang Baoxue, Verkman A S, Kurth Mark J

Abstract excerpt

A developing therapy of cystic fibrosis caused by the DeltaF508 mutation in CFTR employs correction of defective CFTR chloride channel gating by a 'potentiator' and of defective CFTR protein folding by a 'corrector'. Based on SAR data for phenylglycine-type potentiators and bithiazole correctors,...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Source

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Identifiers

PMID: 19954980
DOI: 10.1016/j.bmcl.2009.11.020
PMCID: PMC3165007

Genes

CFTR

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 2 Sept 2026. Prepared record publication-19954980-2026-09-02.2. Manifest publication-graph-cohort-2026-09-02.2.

Source receipt: PubMed via Helena Literature Corpus, retrieved 2 Sept 2026.

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Design and synthesis of a hybrid potentiator-corrector agonist of the cystic fibrosis mutant protein DeltaF508-CFTR.PMID 19954980Read ↗

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Discovery and SAR of 4-aminopyrrolidine-2-carboxylic acid correctors of CFTR for the treatment of cystic fibrosis.Semantic proximity Read ↗

Breakthrough therapies: Cystic fibrosis (CF) potentiators and correctors.Semantic proximity Read ↗

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F508del-cystic fibrosis transmembrane regulator correctors for treatment of cystic fibrosis: a patent review.Semantic proximity Read ↗

Corrector combination therapies for F508del-CFTR.Semantic proximity Read ↗

Nanomolar-potency 'co-potentiator' therapy for cystic fibrosis caused by a defined subset of minimal function CFTR mutants.Semantic proximity Read ↗

A new corrector rescues F508del-CFTR folding through stabilization of the TMD1-NBD1 linkerSemantic proximity Read ↗

Cyanoquinolines with independent corrector and potentiator activities restore ΔPhe508-cystic fibrosis transmembrane conductance regulator chloride channel function in cystic fibrosis.Semantic proximity Read ↗

Towards next generation therapies for cystic fibrosis: Folding, function and pharmacology of CFTR.Semantic proximity Read ↗

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