4gxs

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{{STRUCTURE_4gxs| PDB=4gxs | SCENE= }}
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==Ligand binding domain of GluA2 (AMPA/glutamate receptor) bound to (-)-kaitocephalin==
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===Ligand binding domain of GluA2 (AMPA/glutamate receptor) bound to (-)-kaitocephalin===
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<StructureSection load='4gxs' size='340' side='right' caption='[[4gxs]], [[Resolution|resolution]] 1.96&Aring;' scene=''>
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{{ABSTRACT_PUBMED_23076153}}
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4gxs]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4GXS OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4GXS FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0YS:(5R)-2-[(1S,2R)-2-AMINO-2-CARBOXY-1-HYDROXYETHYL]-5-{(2S)-2-CARBOXY-2-[(3,5-DICHLORO-4-HYDROXYBENZOYL)AMINO]ETHYL}-L-PROLINE'>0YS</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">Glur2, Gria2, Gria2; GluA2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Rattus norvegicus])</td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4gxs FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4gxs OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4gxs RCSB], [http://www.ebi.ac.uk/pdbsum/4gxs PDBsum]</span></td></tr>
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</table>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Glutamate receptors mediate the majority of excitatory synaptic transmission in the central nervous system and excessive stimulation of these receptors is involved in a variety of neurological disorders and neuronal damage from stroke. The development of new subtype specific antagonists would be of considerable therapeutic interest. Natural products can provide important new lead compounds for drug discovery. The only natural product known to inhibit glutamate receptors competitively is (-)-kaitocephalin, which was isolated from the fungus, Eupenicillium shearii and found to protect CNS neurons from excitotoxicity. Previous work has shown that it is a potent antagonist of some subtypes of glutamate receptors (AMPA and NMDA, but not kainate). The structure of kaitocephalin bound to the ligand-binding domain of the AMPA receptor subtype, GluA2, is reported here. The structure suggests how kaitocephalin can be used as a scaffold to develop more selective and high affinity antagonists for glutamate receptors.
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==Function==
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The Structure of (-)-Kaitocephalin Bound to the Ligand Binding Domain of the AMPA/Glutamate Receptor, GluA2.,Ahmed AH, Hamada M, Shinada T, Ohfune Y, Weerasinghe L, Garner PP, Oswald RE J Biol Chem. 2012 Oct 17. PMID:23076153<ref>PMID:23076153</ref>
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[[http://www.uniprot.org/uniprot/GRIA2_RAT GRIA2_RAT]] Receptor for glutamate that functions as ligand-gated ion channel in the central nervous system and plays an important role in excitatory synaptic transmission. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse. The receptor then desensitizes rapidly and enters a transient inactive state, characterized by the presence of bound agonist. In the presence of CACNG4 or CACNG7 or CACNG8, shows resensitization which is characterized by a delayed accumulation of current flux upon continued application of glutamate.<ref>PMID:9351977</ref> <ref>PMID:19265014</ref> <ref>PMID:21172611</ref> <ref>PMID:12501192</ref> <ref>PMID:12015593</ref> <ref>PMID:12872125</ref> <ref>PMID:12730367</ref> <ref>PMID:16192394</ref> <ref>PMID:15591246</ref> <ref>PMID:17018279</ref> <ref>PMID:16483599</ref> <ref>PMID:19946266</ref> <ref>PMID:21317873</ref> <ref>PMID:21846932</ref>
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==About this Structure==
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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[[4gxs]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4GXS OCA].
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</div>
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==Reference==
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==See Also==
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<ref group="xtra">PMID:023076153</ref><references group="xtra"/><references/>
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*[[Ionotropic Glutamate Receptors|Ionotropic Glutamate Receptors]]
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== References ==
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<references/>
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__TOC__
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</StructureSection>
[[Category: Rattus norvegicus]]
[[Category: Rattus norvegicus]]
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[[Category: Ahmed, A H.]]
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[[Category: Ahmed, A H]]
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[[Category: Oswald, R E.]]
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[[Category: Oswald, R E]]
[[Category: Ampa receptor]]
[[Category: Ampa receptor]]
[[Category: Glua2]]
[[Category: Glua2]]

Revision as of 10:52, 21 December 2014

Ligand binding domain of GluA2 (AMPA/glutamate receptor) bound to (-)-kaitocephalin

4gxs, resolution 1.96Å

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