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

Tan, Kelly R; Baur, Roland; Gonthier, Anne; Goeldner, Maurice; 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. 4718-22. Amsterdam: Elsevier 10.1016/j.febslet.2007.08.068

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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.

Item Type:	Journal Article (Original Article)
Division/Institute:	04 Faculty of Medicine > Pre-clinic Human Medicine > Institute of Biochemistry and Molecular Medicine
UniBE Contributor:	Sigel, Erwin
ISSN:	0014-5793
ISBN:	17854801
Publisher:	Elsevier
Language:	English
Submitter:	Factscience Import
Date Deposited:	04 Oct 2013 14:53
Last Modified:	05 Dec 2022 14:16
Publisher DOI:	10.1016/j.febslet.2007.08.068
PubMed ID:	17854801
Web of Science ID:	000250102900029
URI:	https://boris.unibe.ch/id/eprint/22707 (FactScience: 36105)