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The organizing principle of GABA B receptor complexes: Physiological and pharmacological implications
Author(s) -
Fritzius Thorsten,
Bettler Bernhard
Publication year - 2020
Publication title -
basic and clinical pharmacology and toxicology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.805
H-Index - 90
eISSN - 1742-7843
pISSN - 1742-7835
DOI - 10.1111/bcpt.13241
Subject(s) - receptor , obligate , neurotransmission , biology , neurotransmitter receptor , heterologous expression , microbiology and biotechnology , effector , neuroscience , 5 ht2 receptor , neurotransmitter , computational biology , biochemistry , 5 ht receptor , recombinant dna , gene , ecology , serotonin
Abstract GABA B receptors (GBRs), the G protein‐coupled receptors for the neurotransmitter γ‐aminobutyric acid (GABA), regulate synaptic transmission at most synapses in the brain. Proteomic approaches revealed that native GBR complexes assemble from an inventory of ~30 proteins that provide a molecular basis for the functional diversity observed with these receptors. Studies with reconstituted GBR complexes in heterologous cells and complementary knockout studies have allowed to identify cellular and physiological functions for obligate and several non‐obligate receptor components. It emerges that modular association of receptor components in space and time generates a variety of multiprotein receptor complexes with different localizations, kinetic properties and effector channels. This article summarizes current knowledge on the organizing principle of GBR complexes. We further discuss unanticipated receptor functions, links to disease and opportunities for drug discovery arising from the identification of novel receptor components.