Regulation of GABAARs by Transmembrane Accessory Proteins

The vast majority of fast inhibitory transmission in the brain is mediated by GABA acting on GABA(A) receptors (GABA(A)Rs), which provides inhibitory balance to excitatory drive and controls neuronal output. GABA(A)Rs are also effectively targeted by clinically important drugs for treatment in a number of neurological disorders. It has long been hypothesized that function and pharmacology of GABA(A)Rs are determined by the channel pore-forming subunits. However, recent studies have provided new dimensions in studying GABA(A)Rs due to several transmembrane proteins that interact with GABA(A)Rs and modulate their trafficking and function. In this review, we summarize recent findings on these novel GABA(A)R transmembrane regulators and highlight a potential avenue to develop new GABA(A)R psychopharmacology by targeting these receptor associated membrane proteins.

Automated summary

The majority of fast inhibitory transmission in the brain is mediated by GABA acting on GABA(A) receptors, providing inhibitory balance to excitatory drive. Recent studies have revealed that transmembrane proteins interact with GABA(A)Rs and modulate their function and trafficking, offering new dimensions in studying GABA(A)Rs. Targeting these receptor associated membrane proteins may lead to the development of new GABA(A)R psychopharmacology.