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Discovery of Homobivalent Bitopic Ligands Of The Cannabinoid Cb2 Receptor

Authors: Paula Morales; Gemma Navarro; Marc Gómez‐Autet; Laura Redondo; Javier Fernández‐Ruiz; Laura Pérez‐Benito; Arnau Cordomí; +3 Authors

Discovery of Homobivalent Bitopic Ligands Of The Cannabinoid Cb2 Receptor

Abstract

Abstract Single chemical entities with potential to simultaneously interact with two binding sites are emerging strategies in medicinal chemistry. We have designed, synthesized and functionally characterized the first bitopic ligands for the CB 2 receptor. These compounds selectively target CB 2 versus CB 1 receptors. Their binding mode was studied by molecular dynamic simulations and site‐directed mutagenesis.

Country
Spain
Keywords

Proteïnes G, Molecular dynamics, Molecular Dynamics Simulation, Ligands, Receptor, Cannabinoid, CB2, GPCR, G protein-coupled receptors, Cànnabis, Cell receptors, Cannabis, Site-directed mutagenesis, Interacció cel·lular, Binding Sites, CB2 cannabinoid, molecular dynamics, Communications, Bitopic ligand, Cell interaction, Mutagenesis, Site-Directed, bitopic ligands, Receptors cel·lulars, G Proteins, site-directed mutagenesis

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selected citations
These citations are derived from selected sources.
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
views
OpenAIRE UsageCountsViews provided by UsageCounts
downloads
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22
Top 10%
Average
Top 10%
120
139
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