GABAA receptor family: overview on structural characterization

Future Medicinal Chemistry
María Julia AmundarainAlejandro Giorgetti

Abstract

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.

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Citations

Mar 24, 2020·Expert Opinion on Therapeutic Patents·Letizia Crocetti, Gabriella Guerrini
Jun 4, 2020·Computational and Structural Biotechnology Journal·Filippo BaldessariAlejandro Giorgetti
Jun 2, 2021·Cellular and Molecular Life Sciences : CMLS·Erwan SallardPascal Legendre

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Methods Mentioned

BETA
electron microscopy
x-ray
x-ray crystallography
x-ray diffraction

Software Mentioned

Chimera
cEM

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