Structural Basis of GABAB Receptor Regulation and Signaling

Curr Top Behav Neurosci. 2022:52:19-37. doi: 10.1007/7854_2020_147.

Abstract

GABAB receptors (GBRs), the G protein-coupled receptors for the inhibitory neurotransmitter γ-aminobutyric acid (GABA), activate Go/i-type G proteins that regulate adenylyl cyclase, Ca2+ channels, and K+ channels. GBR signaling to enzymes and ion channels influences neuronal activity, plasticity processes, and network activity throughout the brain. GBRs are obligatory heterodimers composed of GB1a or GB1b subunits with a GB2 subunit. Heterodimeric GB1a/2 and GB1b/2 receptors represent functional units that associate in a modular fashion with regulatory, trafficking, and effector proteins to generate receptors with distinct physiological functions. This review summarizes current knowledge on the structure, organization, and functions of multi-protein GBR complexes.

Keywords: AJAP-1; APP; Amyloid precursor protein; GABA-B; HCN; KCTD; PIANP; TRPV1.

Publication types

  • Review

MeSH terms

  • Neurons
  • Receptors, GABA*
  • Receptors, GABA-B*
  • Signal Transduction
  • gamma-Aminobutyric Acid

Substances

  • Receptors, GABA
  • Receptors, GABA-B
  • gamma-Aminobutyric Acid