Dated: May 09, 2023
Publication Name: Nature Communications
Citations : Structural basis for activation of CB1 by an endocannabinoid analog
Endocannabinoids (eCBs) are endogenous ligands of the cannabinoid receptor 1 (CB1), a G protein-coupled receptor that regulates a number of therapeutically relevant physiological responses. Hence, understanding the structural and functional consequences of eCB-CB1 interactions has important implications for designing effective drugs targeting this receptor. To characterize the molecular details of eCB interaction with CB1, we utilized AMG315, an analog of the eCB anandamide to determine the structure of the AMG315-bound CB1 signaling complex. Compared to previous structures, the ligand binding pocket shows some differences.
Contributors: Kaavya Krishna Kumar, Michael J. Robertson, Elina Thadhani, Haoqing Wang, Carl-Mikael Suomivuori, Alexander S. Powers, Lipin Ji, Spyros P. Nikas, Ron O. Dror, Asuka Inoue, Alexandros Makriyannis, Georgios Skiniotis & Brian Kobilka