α₁ Proline 277 Residues Regulate GABA_AR Gating through M2-M3 Loop Interaction in the Interface Region.

ABSTRACT: Cys-loop receptors are a superfamily of transmembrane, pentameric receptors that play a crucial role in mammalian CNS signaling. Physiological activation of these receptors is typically initiated by neurotransmitter binding to the orthosteric binding site, located at the extracellular domain (ECD), which leads to the opening of the channel pore (gate) at the transmembrane domain (TMD). Whereas considerable knowledge on molecular mechanisms of Cys-loop receptor activation was gathered for the acetylcholine receptor, little is known with this respect about the GABA_A receptor (GABA_AR), which mediates cellular inhibition. Importantly, several static structures of GABA_AR were recently described, paving the way to more in-depth molecular functional studies. Moreo

SUBMITTER: Kaczor PT 

PROVIDER: S-EPMC9634794 | biostudies-literature | 2022 Nov

REPOSITORIES: biostudies-literature