Two for the Price of One: Heterobivalent Ligand Design Targeting Two Binding Sites on Voltage-Gated Sodium Channels Slows Ligand Dissociation and Enhances Potency.
Action Potentials
/ drug effects
Amino Acid Sequence
Animals
Binding Sites
Conotoxins
/ chemistry
Cycloaddition Reaction
Humans
Inhibitory Concentration 50
Kinetics
Ligands
Molecular Docking Simulation
NAV1.4 Voltage-Gated Sodium Channel
/ chemistry
NAV1.7 Voltage-Gated Sodium Channel
/ chemistry
Patch-Clamp Techniques
Polyethylenes
/ chemistry
Spider Venoms
/ chemical synthesis
Spiders
/ metabolism
Voltage-Gated Sodium Channel Blockers
/ chemical synthesis
Journal
Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531
Informations de publication
Date de publication:
12 11 2020
12 11 2020
Historique:
pubmed:
21
10
2020
medline:
19
12
2020
entrez:
20
10
2020
Statut:
ppublish
Résumé
Voltage-gated sodium (Na
Identifiants
pubmed: 33078946
doi: 10.1021/acs.jmedchem.0c01107
pmc: PMC7667638
doi:
Substances chimiques
Conotoxins
0
Ligands
0
NAV1.4 Voltage-Gated Sodium Channel
0
NAV1.7 Voltage-Gated Sodium Channel
0
Polyethylenes
0
SCN4A protein, human
0
SCN9A protein, human
0
Spider Venoms
0
Voltage-Gated Sodium Channel Blockers
0
huwentoxin IV, Selenocosmia huwena
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
12773-12785Références
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