Discovery of Homobivalent Bitopic Ligands of the Cannabinoid CB2 Receptor**

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 rec...

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Detalles Bibliográficos
Autores: Morales, Paula, Navarro Brugal, Gemma, Gómez-Autet, Marc, Redondo, Laura, Fernández-Ruiz, Javier, Pérez-Benito, Laura, Cordomí, Arnau, Pardo, Leonardo, Franco Fernández, Rafael, Jagerovic, Nadine
Tipo de recurso: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2020
País:España
Institución:Universidad de Barcelona
Repositorio:Dipòsit Digital de la UB
OAI Identifier:oai:diposit.ub.edu:2445/179068
Acceso en línea:https://hdl.handle.net/2445/179068
Access Level:acceso abierto
Palabra clave:Receptors cel·lulars
Proteïnes G
Interacció cel·lular
Cànnabis
Cell receptors
G Proteins
Cell interaction
Cannabis
Descripción
Sumario: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.

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