Discovery of Homobivalent Bitopic Ligands of the Cannabinoid CB2 Receptor*.
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ABSTRACT:
SUBMITTER: Morales P
PROVIDER: S-EPMC7756656 | biostudies-literature | 2020 Dec
REPOSITORIES: biostudies-literature
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Discovery of Homobivalent Bitopic Ligands of the Cannabinoid CB<sub>2</sub> Receptor*.
Morales Paula P Navarro Gemma G Gómez-Autet Marc M Redondo Laura L Fernández-Ruiz Javier J Pérez-Benito Laura L Cordomí Arnau A Pardo Leonardo L Franco Rafael R Jagerovic Nadine N
Chemistry (Weinheim an der Bergstrasse, Germany) 20201109 68
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<sub>2</sub> receptor. These compounds selectively target CB<sub>2</sub> versus CB<sub>1</sub> receptors. Their binding mode was studied by molecular dynamic simulations and site-directed mutagenesis. ...[more]
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