2YOE

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

Replaces:  4A96

Summary for 2YOE

• Entry DOI: 10.2210/pdb2yoe/pdb
• Related: 2YKS 4A97 4A98
• Descriptor: CYS-LOOP LIGAND-GATED ION CHANNEL, GAMMA-AMINO-BUTANOIC ACID, Flurazepam (3 entities in total)
• Functional Keywords: transport protein, cys-loop receptor, gaba-a receptor, benzodiazepine
• Biological source: ERWINIA CHRYSANTHEMI
• Cellular location: Cell inner membrane; Multi-pass membrane protein (Probable): P0C7B7
• Total number of polymer chains: 10
• Total formula weight: 354427.79

Authors

Spurny, R.,Brams, M.,Nury, H.,Legrand, P.,Ulens, C. (deposition date: 2012-10-23, release date: 2012-10-31, Last modification date: 2023-12-20)

Primary citation

Spurny, R.,Ramerstorfer, J.,Price, K.,Brams, M.,Ernst, M.,Nury, H.,Verheij, M.,Legrand, P.,Bertrand, D.,Bertrand, S.,Dougherty, D.A.,De Esch, I.J.P.,Corringer, P.,Sieghart, W.,Lummis, S.C.R.,Ulens, C.
Pentameric Ligand-Gated Ion Channel Elic is Activated by Gaba and Modulated by Benzodiazepines.
Proc.Natl.Acad.Sci.USA, 109:E3028-, 2012

PubMed Abstract: 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.

PubMed: 23035248
DOI: 10.1073/PNAS.1208208109

Experimental method

X-RAY DIFFRACTION (3.9 Å)