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

Bioorganic & Medicinal Chemistry Letters

Dec 3, 2014

Long YeMark J Kurth

Abstract

The most common mutation causing cystic fibrosis (CF) is deletion of phenylalanine residue 508 in the cystic fibrosis transmembrane regulator conductance (CFTR) protein. Small molecules that are able to correct the misfolding of defective ΔF508-CFTR have considerable promise for therapy...read more

Mentioned in this Paper

Thermodynamics
Structure-Activity Relationship
Molecular Modeling
Analog
Gene Deletion Abnormality
Cystic Fibrosis
Integral to Membrane
Plasma Protein Binding Capacity
Cystic fibrosis transmembrane conductance regulator delta F508
Oxazoles
Paper Details
References

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

Bioorganic & Medicinal Chemistry Letters

Dec 3, 2014

Long YeMark J Kurth

PMID: 25452003

DOI: 10.1016/j.bmcl.2014.09.067

Abstract

The most common mutation causing cystic fibrosis (CF) is deletion of phenylalanine residue 508 in the cystic fibrosis transmembrane regulator conductance (CFTR) protein. Small molecules that are able to correct the misfolding of defective ΔF508-CFTR have considerable promise for therapy...read more

Mentioned in this Paper

Thermodynamics
Structure-Activity Relationship
Molecular Modeling
Analog
Gene Deletion Abnormality
Cystic Fibrosis
Integral to Membrane
Plasma Protein Binding Capacity
Cystic fibrosis transmembrane conductance regulator delta F508
Oxazoles

Related Papers

Paper Details
References
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