Discovery of Homobivalent Bitopic Ligands Of The Cannabinoid Cb2 Receptor

01 July 2020, Version 1
This content is a preprint and has not undergone peer review at the time of posting.


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 CB2 receptor. These compounds selectively target CB2 versus CB1 receptors. Their binding mode was studied by molecular dynamic simulations and site-directed mutagenesis


G protein-coupled receptors
cannabinoid CB2 receptors
bitopic ligands
binding affinity
site-directed mutagenesis
molecular dynamic


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