Binding Modes and Selectivity of Cannabinoid 1 (CB1) and Cannabinoid 2 (CB2) Receptor Ligands.

ABSTRACT: The cannabinoid (CB) receptors (CB₁R and CB₂R) represent a promising therapeutic target for several indications such as nociception and obesity. The ligands with nonselectivity can be traced to the high similarity in the binding sites of both cannabinoid receptors. Therefore, the need for selectivity, potency, and G-protein coupling bias has further complicated the design of desired compounds. The bias of currently studied cannabinoid agonists is seldom investigated, and agonists that do exhibit bias are typically nonselective. However, certain long-chain endocannabinoids represent a class of selective and potent CB₁R agonists. The binding mode for this class of compounds has remained elusive, limiting the implementation of its binding features to currently

SUBMITTER: Yang JF 

PROVIDER: S-EPMC7756905 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature