Fig. 2: Endocannabinoid analog, AMG315-bound CB1–Gi1 structure.
From: Structural basis for activation of CB1 by an endocannabinoid analog
a GTP turnover assay with Gi1 showing maximum turnover produced by FUB (MDMB-Fubinaca) and CP (CP 55940). Endocannabinoid produce much lower GTP turnover compared to their analogs. Data represented as mean ± SD, p < 0.0001****, unpaired t-test (two-tailed), n = 3 independent experiments). b Addition of the PAM, ZCZ increases GTP turnover of the endocannabinoid analogs. (mean ± SD, p < 0.0001****, unpaired t-test (two-tailed), n = 3 independent experiments). c AMG315 binding pocket showing residues that are within 4 Å from the ligand. d. Overlay of ligands from different chemical classes, synthetic cannabinoid (FUB, orange), classical cannabinoid (AM841, green), and endocannabinoid (AMG315, blue).
