GPCRs in VR: Identification of Cannabinoid CB1 Receptor Allosteric Sites to Treat Epilepsy

In this video, we explore new potential ways to treat epilepsy through targeting the cannabinoid 1 receptor (CB1R), which is one of the most widely expressed G protein-coupled receptors (GPCRs) in the brain. The goal of this work was to identify binding sites for GAT228 (R), a partial allosteric agonist, and GAT229 (S), a positive allosteric modulator (PAM) at the CB1R. The study suggests that GAT228 binds in an intracellular exosite that would allow this compound to act as a CB1 allosteric agonist as well as a CB1 PAM. In contrast, GAT229 binds at the extracellular ends of transmembrane helix 2/3, just beneath the extracellular loop 1. At this site, this compound can act as CB1 positive allosteric modulator only. Thanks to our guest speaker Asher Brandt, molecular pharmacology PhD student at the University of Saskatchewan, Canada, who runs his own YouTube channel dedicated to the chemistry of psychedelics: References: Hurst et al. (2019). Identification of CB1 Receptor Allosteric Sites Using Force-Biased MMC Simulated Annealing and Validation by Structure–Activity Relationship Studies. ACS Med. Chem. Lett. 10, 1216−1221 DOWNLOAD NANOME FOR FREE Oculus: Steam: Viveport: SideQuest: SUPPORTED VR HEADSETS Oculus Rift Oculus Quest HTC Vive Complete list: CONNECT WITH US Twitter: LinkedIn: Facebook: Instagram: ABOUT NANOME Website: Step into Nanome and experience the world at the molecular level. From drug discovery to chemistry class, Nanome is a powerful tool for research and education. Visualize, design, and simulate chemical compounds, proteins, and nucleic acids like never before. Collaborate remotely in real-time, save workspaces, and share. Leading pharmaceutical and biotech companies use Nanome to accelerate drug discovery and collaborate with distributed teams across the globe. Educators at top universities use Nanome to teach chemistry in virtual reality, allowing students to explore shapes of proteins and drug compounds and to learn how these structures explain function. Be sure to also check out our blockchain platform, Matryx, which will serve as the backend IP tracking mechanism for Nanome. More info at