Discovery of Homobivalent Bitopic Ligands Of The Cannabinoid Cb2 Receptor

Paula Morales; Gemma Navarro; Marc Gómez-Autet; Laura Redondo; Javier Fernandez-Ruiz; Laura Pérez-Benito; Arnau Cordomí; Leonardo Pardo; Rafael Franco; Nadine Jagerovic

doi:10.26434/chemrxiv.12583604.v1

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Discovery of Homobivalent Bitopic Ligands Of The Cannabinoid Cb2 Receptor

01 July 2020, Version 1

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

Keywords

G protein-coupled receptors

cannabinoid CB2 receptors

bitopic ligands

binding affinity

site-directed mutagenesis

molecular dynamic

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Discovery of Homobivalent Bitopic Ligands of the Cannabinoid CB 2 Receptor**

Paula Morales, Gemma Navarro, Marc Gómez‐Autet, Laura Redondo, Javier Fernández‐Ruiz, Laura Pérez‐Benito, Arnau Cordomí, Leonardo Pardo, Rafael Franco, Nadine Jagerovic journal article

Chemistry – A European Journal , Volume 26, Issue 68

Online publication date: Nov 09, 2020

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Jul 01, 2020 Version 1

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DOI

10.26434/chemrxiv.12583604.v1

Author’s competing interest statement

No conflict of interest

Discovery of Homobivalent Bitopic Ligands Of The Cannabinoid Cb2 Receptor

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Abstract

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