Design, synthesis and biological evaluation of novel orthosteric-allosteric ligands of the cannabinoid receptor type 2 (CB2R)

Design, synthesis and biological evaluation of novel orthosteric-allosteric ligands of the cannabinoid receptor type 2 (CB2R)

It is well known that G protein–coupled receptors (GPCRs) assume multiple active states. Orthosteric ligands and/or allosteric modulators can preferentially stabilize specific conformations, giving rise to pathway-biased signaling. One of the most promising strategies to expand the repertoire of sig...

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Bibliographic Details
Main Authors: Rebecca Ferrisi, Francesca Gado, Beatrice Polini, Caterina Ricardi, Kawthar A. Mohamed, Lesley A. Stevenson, Gabriella Ortore, Simona Rapposelli, Giuseppe Saccomanni, Roger G. Pertwee, Robert B. Laprairie, Clementina Manera, Grazia Chiellini
Format: Article
Language:English
Published: Frontiers Media S.A. 2022-09-01
Series:Frontiers in Chemistry
Subjects:
cannabinoid receptor type 2 (CB2R)
CB2R allosteric modulators
dualsteric agents
antiinflammatory activity
human microglial cells
Online Access:https://www.frontiersin.org/articles/10.3389/fchem.2022.984069/full

Internet

https://www.frontiersin.org/articles/10.3389/fchem.2022.984069/full

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