Pharmacological modulation of GABAA receptors

Ligand-gated ion channels are integral membrane proteins that activate through a change in conformation upon transmitter binding and were identified as key players of brain function. GABA(A) receptors are major inhibitory ligand-gated ion channels of this protein family. They are the target of many therapeutic compounds widely used in the clinic and continue to attract the attention of academic and pharmaceutical laboratories. Advances in the knowledge of the structure of GABA(A) receptors at the molecular level with unprecedented resolution enabled the determination of the binding sites of many allosteric modulators revealing the nature of their interactions with the receptors. Herein, we review the latest findings on allosteric modulation of GABA(A) receptors and their relevance to drug discovery.

Automated summary

GABA(A) receptors are key inhibitory ligand-gated ion channels that are targeted by therapeutic compounds, attracting attention for drug discovery efforts. Recent advances in understanding the molecular structure of these receptors have provided insights into allosteric modulation and its relevance for drug development.