2XQ5: Pentameric Ligand Gated Ion Channel Glic In Complex With Tetraethylarsonium (Teas)

Citation:
Abstract
The flow of ions through cation-selective members of the pentameric ligand-gated ion channel family is inhibited by a structurally diverse class of molecules that bind to the transmembrane pore in the open state of the protein. To obtain insight into the mechanism of channel block, we have investigated the binding of positively charged inhibitors to the open channel of the bacterial homolog GLIC by using X-ray crystallography and electrophysiology. Our studies reveal the location of two regions for interactions, with larger blockers binding in the center of the membrane and divalent transition metal ions binding to the narrow intracellular pore entry. The results provide a structural foundation for understanding the interactions of the channel with inhibitors that is relevant for the entire family.
PDB ID: 2XQ5Download
MMDB ID: 86039
PDB Deposition Date: 2010/9/1
Updated in MMDB: 2010/11
Experimental Method:
x-ray diffraction
Resolution: 3.5  Å
Source Organism:
Similar Structures:
Biological Unit for 2XQ5: pentameric; determined by author and by software (PISA)
Molecular Components in 2XQ5
Label Count Molecule
Proteins (5 molecules)
5
Glr4197 Protein(Gene symbol: glr4197)
Molecule annotation
Chemical (1 molecule)
1
1
* Click molecule labels to explore molecular sequence information.

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