GABA-A receptor structural pharmacology
Supplementary videos from the paper "GABA-A receptor signalling mechanisms revealed by structural pharmacology", authored by Simonas Masiulis, Rooma Desai, Tomasz Uchański, Itziar Serna Martin, Duncan Laverty, Dimple Karia, Tomas Malinauskas, Jasenko Zivanov, Els Pardon, Abhay Kotecha, Jan Steyaert, Keith W. Miller & A. Radu Aricescu, published in Nature (2019) https://doi.org/10.1038/s41586-018-08... | https://www.nature.com/articles/s4158...
Video 1: Structure of the human α1β3γ2L GABAAR in complex with picrotoxin (PTX).
Video 2: Picrotoxin binds within the transmembrane pore of the human α1β3γ2L GABAAR. Architecture of the PTX binding site.
Video 3: Structure of the human α1β3γ2L GABAAR in complex with picrotoxin and GABA.
Video 4: γ-aminobutyric acid (GABA) binding sites in the human α1β3γ2L GABAAR. Close-up of the GABA binding pocket.
Video 5: Conformational differences between picrotoxin- (closed/resting) and picrotoxin/GABA-bound (pre-active) human α1β3γ2L GABAAR structures.
Video 6: Bicuculline (BCC) binding sites in the human α1β3γ2L GABAAR.
Video 7: Structure of the human α1β3γ2L GABAAR in complex with alprazolam (Xanax) and GABA.
Video 8: Alprazolam (Xanax) and diazepam (Valium) binding modes in the α1β3γ2L GABAAR benzodiazepine pocket.
Video 9: Secondary (low affinity) binding site of diazepam (Valium) in the human α1β3γ2L GABAAR transmembrane region.
Video 10: Conformational differences between picrotoxin- (closed/resting) and alprazolam/GABA-bound (desensitized) human α1β3γ2L GABAAR structures.
More information on the paper https://www.nature.com/articles/s4158...