Discovery of Homobivalent Bitopic Ligands of the Cannabinoid CB(2) 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 CB(2) receptor. These compounds selectively target CB(2) versus CB(...

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Detalles Bibliográficos
Autores principales: Morales, Paula, Navarro, Gemma, Gómez‐Autet, Marc, Redondo, Laura, Fernández‐Ruiz, Javier, Pérez‐Benito, Laura, Cordomí, Arnau, Pardo, Leonardo, Franco, Rafael, Jagerovic, Nadine
Formato: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley and Sons Inc. 2020
Materias:
Communications
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7756656/
https://www.ncbi.nlm.nih.gov/pubmed/32794211
http://dx.doi.org/10.1002/chem.202003389
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 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.

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