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Crystal structure of human GABAA receptor

The crystal structure of the human GABAA receptor could help guide the design of new g-aminobutyric acid (GABA)-targeted therapies to treat psychiatric disorders. In vitro, the X-ray crystal structure of the human GABAA receptor bound to the previously unknown agonist benzamidine was solved at a resolution of 3 Å and revealed a complex of 19 different subunits arranged in a homopentameric architecture. The crystal structure also showed that the receptor's neurotransmitter-binding pocket is located between extracellular domains. Next steps include solving the crystal structure of additional heterometric human receptors and evaluating benzamidine derivatives as modulators of such receptors.

SciBX 7(26); doi:10.1038/scibx.2014.778
Published online July 10, 2014

Patent application filed; available for licensing from Isis Innovation Ltd.
Contact: Louis Pymar, Isis Innovation Ltd., Oxford, U.K.
e-mail:
louis.pymar@isis.ox.ac.uk

Miller, P.S. & Aricescu, A.R. Nature; Published online July 8, 2014;
doi:10.1038/nature13293
Contact: A. Radu Aricescu, University of Oxford, Oxford, U.K.
e-mail:
radu@strubi.ox.ac.uk
Contact: Paul Miller, same affiliation as above
e-mail:
paul@strubi.ox.ac.uk