| First Author | Ghit A | Year | 2021 |
| Journal | J Genet Eng Biotechnol | Volume | 19 |
| Issue | 1 | Pages | 123 |
| PubMed ID | 34417930 | Mgi Jnum | J:354418 |
| Mgi Id | MGI:7734812 | Doi | 10.1186/s43141-021-00224-0 |
| Citation | Ghit A, et al. (2021) GABA(A) receptors: structure, function, pharmacology, and related disorders. J Genet Eng Biotechnol 19(1):123 |
| abstractText | BACKGROUND: gamma-Aminobutyric acid sub-type A receptors (GABA(A)Rs) are the most prominent inhibitory neurotransmitter receptors in the CNS. They are a family of ligand-gated ion channel with significant physiological and therapeutic implications. MAIN BODY: GABA(A)Rs are heteropentamers formed from a selection of 19 subunits: six alpha (alpha1-6), three beta (beta1-3), three gamma (gamma1-3), three rho (rho1-3), and one each of the delta (delta), epsilon (epsilon), pi (pi), and theta (theta) which result in the production of a considerable number of receptor isoforms. Each isoform exhibits distinct pharmacological and physiological properties. However, the majority of GABA(A)Rs are composed of two alpha subunits, two beta subunits, and one gamma subunit arranged as gamma2beta2alpha1beta2alpha1 counterclockwise around the center. The mature receptor has a central chloride ion channel gated by GABA neurotransmitter and modulated by a variety of different drugs. Changes in GABA synthesis or release may have a significant effect on normal brain function. Furthermore, The molecular interactions and pharmacological effects caused by drugs are extremely complex. This is due to the structural heterogeneity of the receptors, and the existence of multiple allosteric binding sites as well as a wide range of ligands that can bind to them. Notably, dysfunction of the GABAergic system contributes to the development of several diseases. Therefore, understanding the relationship between GABA(A) receptor deficits and CNS disorders thus has a significant impact on the discovery of disease pathogenesis and drug development. CONCLUSION: To date, few reviews have discussed GABA(A) receptors in detail. Accordingly, this review aims to summarize the current understanding of the structural, physiological, and pharmacological properties of GABA(A)Rs, as well as shedding light on the most common associated disorders. |
