Click here to close Hello! We notice that you are using Internet Explorer, which is not supported by Xenbase and may cause the site to display incorrectly. We suggest using a current version of Chrome, FireFox, or Safari.
XB-ART-46543
Proc Natl Acad Sci U S A 2012 Oct 30;10944:E3028-34. doi: 10.1073/pnas.1208208109.
Show Gene links Show Anatomy links

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 .


???displayArticle.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.

???displayArticle.pubmedLink??? 23035248
???displayArticle.pmcLink??? PMC3497736
???displayArticle.link??? Proc Natl Acad Sci U S A
???displayArticle.grants??? [+]


References [+] :
Amin, Two tyrosine residues on the alpha subunit are crucial for benzodiazepine binding and allosteric modulation of gamma-aminobutyric acidA receptors. 1997, Pubmed, Xenbase