Pharmacological modulation of GABAA receptors.

Frédéric Knoflach, Daniel Bertrand

Current opinion in pharmacology 2021 Aug

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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. GABAA 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 GABAA 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 GABAA receptors and their relevance to drug discovery. Copyright © 2021 Elsevier Ltd. All rights reserved.