In Search of GABAA Receptor's Neurosteroid Binding Sites

Neurosteroids (NS) are the main modulators of γ-aminobutyric acid type A receptors (GABAARs), which are the ligand-gated channels target of the major inhibitory neurotransmitter in vertebrates. As a consequence of their ability to modify inhibitory functions in the brain, NS have high physiological...

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Publicado: 2018
Acceso en línea:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00222623_v_n_p_Alvarez
http://hdl.handle.net/20.500.12110/paper_00222623_v_n_p_Alvarez
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Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) de Universidad de Buenos Aires
id paper:paper_00222623_v_n_p_Alvarez
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spelling paper:paper_00222623_v_n_p_Alvarez2023-06-08T14:48:39Z In Search of GABAA Receptor's Neurosteroid Binding Sites Neurosteroids (NS) are the main modulators of γ-aminobutyric acid type A receptors (GABAARs), which are the ligand-gated channels target of the major inhibitory neurotransmitter in vertebrates. As a consequence of their ability to modify inhibitory functions in the brain, NS have high physiological and clinical relevance. Accumulated evidence has strongly suggested that NS binding sites were located in the GABAAR transmembrane domain; however the specific localization of these sites has remained an enigma for decades. Fortunately, recent resolution of GABAARs crystal structures, together with computational strategies applied to investigate the NS binding, has paved the way to rationalizing the molecular basis of NS modulation. This work reviews from a historical perspective the road followed for establishing the GABAAR/NS binding mode, from their initial molecular modeling to the latest findings. Furthermore, a comparative analysis describing the NS binding is provided, plus a preliminary analysis of putative NS sites in other assemblies. © 2018 American Chemical Society. 2018 https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00222623_v_n_p_Alvarez http://hdl.handle.net/20.500.12110/paper_00222623_v_n_p_Alvarez
institution Universidad de Buenos Aires
institution_str I-28
repository_str R-134
collection Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA)
description Neurosteroids (NS) are the main modulators of γ-aminobutyric acid type A receptors (GABAARs), which are the ligand-gated channels target of the major inhibitory neurotransmitter in vertebrates. As a consequence of their ability to modify inhibitory functions in the brain, NS have high physiological and clinical relevance. Accumulated evidence has strongly suggested that NS binding sites were located in the GABAAR transmembrane domain; however the specific localization of these sites has remained an enigma for decades. Fortunately, recent resolution of GABAARs crystal structures, together with computational strategies applied to investigate the NS binding, has paved the way to rationalizing the molecular basis of NS modulation. This work reviews from a historical perspective the road followed for establishing the GABAAR/NS binding mode, from their initial molecular modeling to the latest findings. Furthermore, a comparative analysis describing the NS binding is provided, plus a preliminary analysis of putative NS sites in other assemblies. © 2018 American Chemical Society.
title In Search of GABAA Receptor's Neurosteroid Binding Sites
spellingShingle In Search of GABAA Receptor's Neurosteroid Binding Sites
title_short In Search of GABAA Receptor's Neurosteroid Binding Sites
title_full In Search of GABAA Receptor's Neurosteroid Binding Sites
title_fullStr In Search of GABAA Receptor's Neurosteroid Binding Sites
title_full_unstemmed In Search of GABAA Receptor's Neurosteroid Binding Sites
title_sort in search of gabaa receptor's neurosteroid binding sites
publishDate 2018
url https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00222623_v_n_p_Alvarez
http://hdl.handle.net/20.500.12110/paper_00222623_v_n_p_Alvarez
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