Direct Structural Insights into GABAA Receptor Pharmacology

Jeong Joo Kim, Ryan E. Hibbs

Research output: Contribution to journalReview articlepeer-review

Abstract

GABAA receptors are pentameric ligand-gated ion channels that mediate most fast neuronal inhibition in the brain. In addition to their important physiological roles, they are noteworthy in their rich pharmacology; prominent drugs used for anxiety, insomnia, and general anesthesia act through positive modulation of GABAA receptors. Direct structural information for how these drugs work was absent until recently. Efforts in structural biology over the past few years have revealed how important drug classes and natural products interact with the GABAA receptor, providing a foundation for studies in dynamics and structure-guided drug design. Here, we review recent developments in GABAA receptor structural pharmacology, focusing on subunit assemblies of the receptor found at synapses.

Original languageEnglish (US)
Pages (from-to)502-517
Number of pages16
JournalTrends in biochemical sciences
Volume46
Issue number6
DOIs
StatePublished - Jun 2021

Keywords

  • benzodiazepine
  • bicuculline
  • cryo-EM structure
  • Cys-loop receptor structure
  • general anesthetic
  • picrotoxin

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology

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