Structural basis of the activation of a metabotropic GABA receptor.

ABSTRACT: Metabotropic γ-aminobutyric acid receptors (GABA_B) are involved in the modulation of synaptic responses in the central nervous system and have been implicated in neuropsychological conditions that range from addiction to psychosis¹. GABA_B belongs to class C of the G-protein-coupled receptors, and its functional entity comprises an obligate heterodimer that is composed of the GB1 and GB2 subunits². Each subunit possesses an extracellular Venus flytrap domain, which is connected to a canonical seven-transmembrane domain. Here we present four cryo-electron microscopy structures of the human full-length GB1-GB2 heterodimer: one structure of its inactive apo state, two intermediate agonist-bound forms and an active form in which the heterodimer is bou

SUBMITTER: Shaye H 

PROVIDER: S-EPMC8020835 | biostudies-literature | 2020 Aug

REPOSITORIES: biostudies-literature