Cryo-electron microscopy reveals informative details of GABA_A receptor structural pharmacology: implications for drug discovery

The first cryoEM high-resolution structure of a recombinant full-length heterotrimeric γ-aminobutyric acid (GABA) type A receptor (GABAR) subtype α1β3γ2L in complex with important GABAR ligands was published by the Aricescu lab in January 2019 (1,2). GABARs are the major receptors mediating rapid inhibitory neurotransmission in the central nervous system and members of the pentameric ligand-gated ion channel (pLGIC) gene superfamily.