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RSS FeedsMarine Drugs, Vol. 17, Pages 303: Blockade of Human ?7 Nicotinic Acetylcholine Receptor by ?-Conotoxin ImI Dendrimer: Insight from Computational Simulations (Marine Drugs)

 
 

23 may 2019 19:00:22

 
Marine Drugs, Vol. 17, Pages 303: Blockade of Human ?7 Nicotinic Acetylcholine Receptor by ?-Conotoxin ImI Dendrimer: Insight from Computational Simulations (Marine Drugs)
 




Nicotinic acetylcholine receptors (nAChRs) are ligand-gated ion channels that are involved in fast synaptic transmission and mediated physiological activities in the nervous system. α-Conotoxin ImI exhibits subtype-specific blockade towards homomeric α7 and α9 receptors. In this study, we established a method to build a 2×ImI-dendrimer/h (human) α7 nAChR model, and based on this model, we systematically investigated the molecular interactions between the 2×ImI-dendrimer and hα7 nAChR. Our results suggest that the 2×ImI-dendrimer possessed much stronger potency towards hα7 nAChR than the α-ImI monomer and demonstrated that the linker between α-ImI contributed to the potency of the 2×ImI-dendrimer by forming a stable hydrogen-bond network with hα7 nAChR. Overall, this study provides novel insights into the binding mechanism of α-ImI dendrimer to hα7 nAChR, and the methodology reported here opens an avenue for the design of more selective dendrimers with potential usage as drug/gene carriers, macromolecular drugs, and molecular probes.


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33 viewsCategory: Biochemistry, Molecular Biology, Pharmacology
 
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