Glycine receptors in GtoPdb v.2021.3

The inhibitory glycine receptor (nomenclature as agreed by the NC-IUPHAR Subcommittee on Glycine Receptors) is a member of Cys-loop superfamily transmitter-gated ion channels that includes zinc activated channels, GABAA, nicotinic acetylcholine and 5-HT3 receptors Zn2+- channels. expressed either homo-pentamer α subunits, or complex now thought to harbour 2α 3β subunits [33, 7], contain an intrinsic anion channel. Four differentially isoforms α-subunit (α1-α4) one variant β-subunit (β1, GLRB, P48167) have been identified genomic cDNA cloning. Further diversity originates from alternative splicing primary gene transcripts for α1 (α1INS α1del), α2 (α2A α2B), α3 (α3S α3L) β (βΔ7) mRNA editing subunit [83, 93, 21]. Both can produce (i.e., α2B α3P185L) with enhanced agonist sensitivity. Predominantly, adult form contains (or α3) whereas immature mostly composed only subunits. &a;pha;4 pseudogene in humans. High resolution molecular structures are available homomeric [50, 20]. As other receptors, orthosteric binding site agonists competitive antagonist strychnine formed at interfaces between subunits’ extracellular domains. Inclusion pentameric contributes binding, reduces single channel conductance alters pharmacology. also anchors receptor, via amphipathic sequence within large intracellular loop region, gephyrin. This cytoskeletal attachment protein binds number subsynaptic proteins involved structure thus clusters hetero-oligomeric synapse [56, 54, 88]. G βγ enhance open state probability native recombinant association domains [124, 123]. Intracellular chloride concentration modulates kinetics [96]. Ca2+ appears increase affinity, prolonging events, mechanism does not involve phosphorylation [27]. Extracellular Zn2+ potentiates GlyR function nanomolar concentrations [86]. causes inhibition higher micromolar (17).