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Article

Synergy-based small-molecule screen using a human lung epithelial cell line yields ΔF508-CFTR correctors that augment VX-809 maximal efficacy.

Molecular pharmacology - 1 Jul 2014

Phuan Puay-Wah, Veit Guido, Tan Joseph, Roldan Ariel, Finkbeiner Walter E, Lukacs Gergely L, Verkman A S

Abstract excerpt

The most prevalent cystic fibrosis transmembrane conductance regulator (CFTR) mutation causing cystic fibrosis, ΔF508, impairs folding of nucleotide binding domain (NBD) 1 and stability of the interface between NBD1 and the membrane-spanning domains. The interfacial stability defect can be partia...

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Source

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Identifiers

PMID: 24737137
DOI: 10.1124/mol.114.092478
PMCID: PMC4054004

Genes

CFTR

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 4 Sept 2026. Prepared record publication-24737137-2026-09-04.2. Manifest publication-graph-cohort-2026-09-04.2.

Source receipt: PubMed via Helena Literature Corpus, retrieved 4 Sept 2026.

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Synergy-based small-molecule screen using a human lung epithelial cell line yields ΔF508-CFTR correctors that augment VX-809 maximal efficacy.PMID 24737137Read ↗

Structure-guided combination of novel CFTR correctors to improve the function of F508del-CFTR in airway epithelial cells.Semantic proximity Read ↗

Mechanism-based corrector combination restores ΔF508-CFTR folding and function.Semantic proximity Read ↗

Discovery of novel VX-809 hybrid derivatives as F508del-CFTR correctors by molecular modeling, chemical synthesis and biological assays.Semantic proximity Read ↗

Novel tricyclic pyrrolo-quinolines as pharmacological correctors of the mutant CFTR chloride channel.Semantic proximity Read ↗

Identification of novel F508del-CFTR traffic correctors among triazole derivatives.Semantic proximity Read ↗

Synthesis and biological evaluation of novel thiazole- VX-809 hybrid derivatives as F508del correctors by QSAR-based filtering tools.Semantic proximity Read ↗

Identification of 6,9-dihydro-5H-pyrrolo[3,2-h]quinazolines as a new class of F508del-CFTR correctors for the treatment of cystic fibrosis.Semantic proximity Read ↗

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PTI-801 (posenacaftor) shares a common mechanism with VX-445 (elexacaftor) to rescue p.Phe508del-CFTR.Semantic proximity Read ↗

Small-molecule correctors of defective DeltaF508-CFTR cellular processing identified by high-throughput screening.Semantic proximity Read ↗

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Characterization of the mechanism of action of RDR01752, a novel corrector of F508del-CFTR.Semantic proximity Read ↗

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