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Cannabinoid Receptor in Complex with THC 5XRA

Featured Image

Cannabinoid receptors are part of the endocannabinoid system, which is involved in a variety of physiological processes including appetite, pain-sensation, mood, and memory. This 3D print of THC Cannabinoid Receptor Complex 5TGZ is designed to visualize THC (color by atom type) bound inside the receptor-binding pocket.

Protein Description

Cannabinoid receptors are typical of G protein-coupled receptors containing seven transmembrane spanning domains. Cannabinoid receptors are activated by three major groups of ligands: endocannabinoids, produced by the body; plant cannabinoids (such as Tetrahydrocannabinol or THC, produced by the cannabis plant); and synthetic cannabinoids (such as HU-210). There are currently two known subtypes of cannabinoid receptors, termed CB1 and CB2. The CB1 receptor is expressed mainly in the brain, but also in the lungs, liver, and kidneys. The CB2 receptor is expressed mainly in the immune system and in hematopoietic cells. Cannabinoids bind reversibly to cannabinoid receptors. Subtype selective cannabinoids have been developed which theoretically may have advantages for the treatment of certain diseases such as obesity or infectious diseases.

Cannabinoid Receptors and COVID-19

The protective role of estrogens, as well as an immune-suppressive activity that limits the effects of excessive inflammation and can be mediated by cannabinoid receptor type 2 (CB2). The role of this receptor in modulating inflammation and an immune response is well documented. The stimulation of CB2 receptors is known to limit the release of pro-inflammatory cytokines, shift the macrophage phenotype towards the anti-inflammatory M2 type, while also enhancing the immune-modulating properties of mesenchymal stromal cells. For these reasons, was hypothesize that CB2 receptor can be a therapeutic target in COVID-19 pandemic emergency.

3D Print of Cannabinoid Receptor (tinted green) in Complex with THC (colored by atom type) 5XRA

A novel ∆9-tetrahydrocannabinol (∆9-THCP) binds with high affinity to both human CB1 and CB2 receptors. In particular, the affinity shown for CB1 is thirty-fold higher compared to the one reported for Δ9-THC in the literature, and it was 5 to 10 times more active on the CB2 receptor. More studies are necessary to develop a commercially available CB2 selective agonist, and clinical studies with the available phytocannabinoids should be encouraged.

Biologic Explorer: 5XRA

Explore the protein dataset used to create this 3D printed protein model.

3D Print Cannabinoid Receptor Complex 5XRA

Model Description

This 3D printed protein model of ​THC (Red) Cannabinoid Receptor (Shades of green) Complex. It is visualized as a volumetric surface and colored by the protein’s bFactor. Model created from PDB ID: 5XRA.