4u5g

Crystal structure of con-ikot-ikot toxin

spinqualitylabelsall models 4u5g, resolution 2.20Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 4u5g is a 2 chain structure with sequence from Conus striatus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: X-ray diffraction, Resolution 2.1997Å Ligands: ZN Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function CONII_CONST Publication Abstract from PubMed AMPA-sensitive glutamate receptors are crucial to the structural and dynamical properties of the brain, to the development and function of the central nervous system, and to the treatment of neurological conditions from depression to cognitive impairment. However, the molecular principles underlying AMPA receptor activation have remained elusive. Here, we determine multiple x-ray crystal structures of the GluA2 AMPA receptor in complex with a Conus striatus cone snail toxin, a positive allosteric modulator, and orthosteric agonists, at 3.8 to 4.1 angstrom resolution. We show how the toxin acts like a "straight jacket" on the ligand-binding domain (LBD) "gating ring," restraining the domains via both intra- and interdimer cross-links such that agonist-induced closure of the LBD "clamshells" is transduced into an irislike expansion of the gating ring. By structural analysis of activation-enhancing mutants, we show how the expansion of the LBD gating ring results in "pulling" forces on the M3 helices that, in turn, are coupled to ion channel gating. X-ray structures of AMPA receptor-cone snail toxin complexes illuminate activation mechanism.,Chen L, Duerr KL, Gouaux E Science. 2014 Aug 7. pii: 1258409. PMID:25103405 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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