In Search of GABAA Receptor's Neurosteroid Binding Sites

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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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Autor principal: Alvarez, L.D
Otros Autores: Pecci, A., Estrin, D.A
Formato: Capítulo de libro
Lenguaje:Inglés
Publicado: American Chemical Society 2018
Acceso en línea:Registro en Scopus
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Biblioteca Central Dr. Luis F. Leloir (FCEN) de Universidad de Buenos Aires
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100 1 |a Alvarez, L.D. 
245 1 3 |a In Search of GABAA Receptor's Neurosteroid Binding Sites 
260 |b American Chemical Society  |c 2018 
270 1 0 |m Alvarez, L.D.; Departamento de Química Biológica, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Ciudad UniversitariaArgentina; email: lalvarez@qo.fcen.uba.ar 
506 |2 openaire  |e Política editorial 
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520 3 |a 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.  |l eng 
536 |a Article in Press 
593 |a Departamento de Química Biológica, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Ciudad Universitaria, Buenos Aires, C1428EGA, Argentina 
593 |a Departamento de Química Inorgánica Analítica y Química Física, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Ciudad Universitaria, Buenos Aires, C1428EGA, Argentina 
593 |a UMYMFOR, CONICET, Universidad de Buenos Aires, Ciudad Universitaria, Buenos Aires, C1428EGA, Argentina 
593 |a IFIBYNE, CONICET, Universidad de Buenos Aires, Ciudad Universitaria, Buenos Aires, C1428EGA, Argentina 
593 |a INQUIMAE, CONICET, Universidad de Buenos Aires, Ciudad Universitaria, Buenos Aires, C1428EGA, Argentina 
700 1 |a Pecci, A. 
700 1 |a Estrin, D.A. 
773 0 |d American Chemical Society, 2018  |p J. Med. Chem.  |x 00222623  |w (AR-BaUEN)CENRE-686  |t Journal of Medicinal Chemistry 
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856 4 0 |u https://doi.org/10.1021/acs.jmedchem.8b01400  |y DOI 
856 4 0 |u https://hdl.handle.net/20.500.12110/paper_00222623_v_n_p_Alvarez  |y Handle 
856 4 0 |u https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00222623_v_n_p_Alvarez  |y Registro en la Biblioteca Digital 
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