2XQ3

Pentameric ligand gated ion channel GLIC in complex with Br-lidocaine

Summary for 2XQ3

• Entry DOI: 10.2210/pdb2xq3/pdb
• Related: 2XQ4 2XQ5 2XQ6 2XQ7 2XQ8 2XQ9 2XQA
• Descriptor: GLR4197 PROTEIN, BROMIDE ION (2 entities in total)
• Functional Keywords: membrane protein, open channel block
• Biological source: GLOEOBACTER VIOLACEUS PCC 7421
• Total number of polymer chains: 5
• Total formula weight: 181468.52

Authors

Hilf, R.J.C.,Bertozzi, C.,Zimmermann, I.,Reiter, A.,Trauner, D.,Dutzler, R. (deposition date: 2010-09-01, release date: 2010-11-10, Last modification date: 2024-05-08)

Primary citation

Hilf, R.J.C.,Bertozzi, C.,Zimmermann, I.,Reiter, A.,Trauner, D.,Dutzler, R.
Structural Basis of Open Channel Block in a Prokaryotic Pentameric Ligand-Gated Ion Channel
Nat.Struct.Mol.Biol., 17:1330-, 2010

PubMed 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.

PubMed: 21037567
DOI: 10.1038/NSMB.1933

Experimental method

X-RAY DIFFRACTION (3.5 Å)