GABAA receptor family: overview on structural characterization
| Autor: | Marcelo Daniel Costabel, María Julia Amundarain, Rui Ribeiro, Alejandro Giorgetti |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
Cryo-electron microscopy
Ciencias Físicas COMPARATIVE MODELING CRYO-EM Otras Ciencias Físicas 01 natural sciences Gamma-Aminobutyric Acid Receptor 03 medical and health sciences Drug Discovery HOMOLOGY MODELING Homology modeling Inhibitory transmission Receptor Ion channel GAMMA-AMINOBUTYRIC ACID RECEPTOR 030304 developmental biology Pharmacology GABAAR 0303 health sciences Chemistry GABAA receptor CYS-LOOP RECEPTORS PENTAMERIC LIGAND-GATED ION CHANNELS (PLGICS) 0104 chemical sciences 010404 medicinal & biomolecular chemistry X-RAY CRYSTALLOGRAPHY Biophysics Molecular Medicine STRUCTURE DETERMINATION CIENCIAS NATURALES Y EXACTAS Cys-loop receptors |
| Zdroj: | Future Medicinal Chemistry. 11:229-245 |
| ISSN: | 1756-8927 1756-8919 |
| Popis: | The pentameric γ-aminobutyric acid type A receptors are ion channels activated by ligands, which intervene in the rapid inhibitory transmission in the mammalian CNS. Due to their rich pharmacology and therapeutic potential, it is essential to understand their structure and function thoroughly. This deep characterization was hampered by the lack of experimental structural information for many years. Thus, computational techniques have been extensively combined with experimental data, in order to undertake the study of γ-aminobutyric acid type A receptors and their interaction with drugs. Here, we review the exciting journey made to assess the structures of these receptors and outline major outcomes. Finally, we discuss the brand new structure of the α1β2γ2 subtype and the amazing advances it brings to the field. Fil: Amundarain, María Julia. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Instituto de Física del Sur. Universidad Nacional del Sur. Departamento de Física. Instituto de Física del Sur; Argentina Fil: Ribeiro, Rui Pedro. Universita di Verona; Italia Fil: Costabel, Marcelo Daniel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Instituto de Física del Sur. Universidad Nacional del Sur. Departamento de Física. Instituto de Física del Sur; Argentina Fil: Giorgetti, Alejandro. Institute of Neuroscience and Medicine. Department Computational Biomedicine; Alemania. Universita di Verona; Italia |
| Databáze: | OpenAIRE |
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