Dated: Jun 30, 2022
Publication Name: Biochemical and Biophysical Research Communications
Citations : Cryo-EM structures of the β3 adrenergic receptor bound to solabegron and isoproterenol
The β3-adrenergic receptor (β3AR) is the most essential drug target for overactive bladder and has therapeutic potentials for the treatments of type 2 diabetes and obesity. Here, we report the cryo-electron microscopy structures of the β3AR-Gs signaling complexes with the selective agonist, solabegron and the nonselective agonist, isoproterenol. Comparison of the isoproterenol-, mirabegron-, and solabegron-bound β3AR structures revealed that the extracellular loop 2 changes its conformation depending on the bound agonist and plays an essential role in solabegron binding.
Contributors: Ikko Nureki, Kazuhiro Kobayashi, Tatsuki Tanaka, Kanae Demura, Asuka Inoue, Wataru Shihoya, Osamu Nureki