Discovery of Homobivalent Bitopic Ligands of the Cannabinoid CB Receptor

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Título:	Discovery of Homobivalent Bitopic Ligands of the Cannabinoid CB Receptor
Autor/a:	Morales, Paula; Navarro, Gemma; Gómez-Autet, Marc; Redondo, Laura; Fernández-Ruiz, Javier; Pérez-Benito, Laura; Cordomí Montoya, Arnau; Pardo Carrasco, Leonardo; Franco, Rafael; Jagerovic, Nadine
Abstract:	Altres ajuts: This work was supported bythe CSIC (PIE-201580E033). P.M. is grateful to the CM program "Atracción de Talento Investigador" number 2018-T2/BMD-1081.
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 receptor. These compounds selectively target CB versus CB receptors. Their binding mode was studied by molecular dynamic simulations and site-directed mutagenesis. Single chemical entities with potential to simultaneously interact with two binding sites are emerging strategies in GPCR pharmacology. We present herein the design, synthesis and functional characterization of the first bitopic ligands for the CB receptor. Molecular understanding of the binding mode was guided by molecular dynamic simulations and site-directed mutagenesis.
Materia(s):	-Bitopic ligands -CB2 cannabinoid -G protein-coupled receptors -Molecular dynamics -Site-directed mutagenesis
Derechos:	open access Aquest document està subjecte a una llicència d'ús Creative Commons. Es permet la reproducció total o parcial, la distribució, la comunicació pública de l'obra i la creació d'obres derivades, fins i tot amb finalitats comercials, sempre i quan es reconegui l'autoria de l'obra original. https://creativecommons.org/licenses/by/4.0/
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Uri:	https://ddd.uab.cat/record/238561

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