Direct Binding of the Corrector VX-809 to Human CFTR NBD1: Evidence of an Allosteric Coupling between the Binding Site and the NBD1:CL4 Interface

Understanding the mechanism of action of modulator compounds for the cystic fibrosis transmembrane conductance regulator (CFTR) is key for the optimization of therapeutics as well as obtaining insights into the molecular mechanisms of CFTR function. We demonstrate the direct binding of VX-809 to the...

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Veröffentlicht in:	Molecular pharmacology 2017-08, Vol.92 (2), p.124-135
Hauptverfasser:	Hudson, Rhea P., Dawson, Jennifer E., Chong, P. Andrew, Yang, Zhengrong, Millen, Linda, Thomas, Philip J., Brouillette, Christie G., Forman-Kay, Julie D.
Format:	Artikel
Sprache:	eng
Schlagworte:	Allosteric Regulation - physiology Aminopyridines - chemistry Aminopyridines - metabolism Benzodioxoles - chemistry Benzodioxoles - metabolism Binding Sites - physiology Carrier Proteins - chemistry Carrier Proteins - metabolism Cystic Fibrosis Transmembrane Conductance Regulator - chemistry Cystic Fibrosis Transmembrane Conductance Regulator - metabolism Humans Protein Binding - physiology Protein Structure, Secondary Protein Structure, Tertiary
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