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Two for the Price of One: Heterobivalent Ligand Design Targeting Two Binding Sites on Voltage-Gated Sodium Channels Slows Ligand Dissociation and Enhances Potency

[Image: see text] Voltage-gated sodium (Na(V)) channels are pore-forming transmembrane proteins that play essential roles in excitable cells, and they are key targets for antiepileptic, antiarrhythmic, and analgesic drugs. We implemented a heterobivalent design strategy to modulate the potency, sele...

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Bibliografische gegevens
Gepubliceerd in:J Med Chem
Hoofdauteurs: Peschel, Alicia, Cardoso, Fernanda C., Walker, Andrew A., Durek, Thomas, Stone, M. Rhia L., Braga Emidio, Nayara, Dawson, Philip E., Muttenthaler, Markus, King, Glenn F.
Formaat: Artigo
Taal:Inglês
Gepubliceerd in: American Chemical Society 2020
Online toegang:https://ncbi.nlm.nih.gov/pmc/articles/PMC7667638/
https://ncbi.nlm.nih.gov/pubmed/33078946
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.0c01107
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