GABA-A R beta 1: Small Molecules and Peptides

GABA A (γ-aminobutyric acid-type A) receptors are members of the cysteine-loop family of neurotransmitter-gated ion channels. GABA binding to A-type receptors induces anion-selective ion channel opening. These receptors are the principal fast inhibitory neurotransmitter receptors in the CNS. GABA A receptors are heteropentamer combinations of seven subunit types; α, β, γ, δ, ε, θ, and π. Three subunits, α, β, and γ, have at least three separate gene products in mammals, and typical GABA A receptors have some combination of α, β, and γ subunits.

The rat β1 isoform is a 58 - 60 kDa, 449 amino acid (aa), 4 transmembrane protein with two terminal extracellular regions. The ligand-binding region is in the N-terminus (aa 13 - 218). The β1 subunit is known to be phosphorylated on a consensus phosphorylation site (S409 of the precursor) that exists in the cytoplasmic domain between transmembrane segments 3 and 4. PKA or PKC βII-induced phosphorylation decreases GABA A receptor activity.