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Two neighboring residues of loop A of the alpha1 subunit point towards the benzodiazepine binding site of GABAA receptors

Tan, Kelly R. and Baur, Roland and Gonthier, Anne and Goeldner, Maurice and Sigel, Erwin. (2007) Two neighboring residues of loop A of the alpha1 subunit point towards the benzodiazepine binding site of GABAA receptors. FEBS Letters, 581 (24). pp. 4718-4722.

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Official URL: http://edoc.unibas.ch/50654/

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Abstract

Benzodiazepines are widely used drugs exerting sedative, anxiolytic, muscle relaxant, and anticonvulsant effects by acting through specific high affinity binding sites on some GABA(A) receptors. It is important to understand how these ligands are positioned in this binding site. We are especially interested here in the conformation of loop A of the alpha(1)beta(2)gamma(2) GABA(A) receptor containing a key residue for the interaction of benzodiazepines: alpha(1)H101. We describe a direct interaction of alpha(1)N102 with a diazepam- and an imidazobenzodiazepine-derivative. Our observations help to better understand the conformation of this region of the benzodiazepine pocket in GABA(A) receptor.
Faculties and Departments:05 Faculty of Science > Departement Biozentrum > Neurobiology > Physiopathology of basal ganglia neuronal subcircuits (Tan)
UniBasel Contributors:Tan, Kelly
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:Elsevier
ISSN:0014-5793
e-ISSN:1873-3468
Note:Publication type according to Uni Basel Research Database: Journal article
Identification Number:
Last Modified:28 Nov 2017 08:31
Deposited On:28 Nov 2017 08:31

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