4a98

X-ray structure of a pentameric ligand gated ion channel from Erwinia chrysanthemi (ELIC) in complex with bromoflurazepam

spinqualitylabelsall models 4a98, resolution 3.61Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 4a98 is a 10 chain structure with sequence from Dickeya chrysanthemi. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: X-ray diffraction, Resolution 3.61Å Ligands: BFZ Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function ELIC_DICCH Publication Abstract from PubMed GABA(A) receptors are pentameric ligand-gated ion channels involved in fast inhibitory neurotransmission and are allosterically modulated by the anxiolytic, anticonvulsant, and sedative-hypnotic benzodiazepines. Here we show that the prokaryotic homolog ELIC also is activated by GABA and is modulated by benzodiazepines with effects comparable to those at GABA(A) receptors. Crystal structures reveal important features of GABA recognition and indicate that benzodiazepines, depending on their concentration, occupy two possible sites in ELIC. An intrasubunit site is adjacent to the GABA-recognition site but faces the channel vestibule. A second intersubunit site partially overlaps with the GABA site and likely corresponds to a low-affinity benzodiazepine-binding site in GABA(A) receptors that mediates inhibitory effects of the benzodiazepine flurazepam. Our study offers a structural view how GABA and benzodiazepines are recognized at a GABA-activated ion channel. Pentameric ligand-gated ion channel ELIC is activated by GABA and modulated by benzodiazepines.,Spurny R, Ramerstorfer J, Price K, Brams M, Ernst M, Nury H, Verheij M, Legrand P, Bertrand D, Bertrand S, Dougherty DA, de Esch IJ, Corringer PJ, Sieghart W, Lummis SC, Ulens C Proc Natl Acad Sci U S A. 2012 Oct 3. PMID:23035248 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Ion channels 3D structures

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