View source for 4tk2


==Geph E in complex with a GABA receptor alpha3 subunit derived peptide in space group P61==
<StructureSection load='4tk2' size='340' side='right'caption='[[4tk2]], [[Resolution|resolution]] 4.10&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[4tk2]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Buffalo_rat Buffalo rat]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4TK2 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4TK2 FirstGlance]. <br>
</td></tr><tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[2fu3|2fu3]], [[2fts|2fts]], [[4pdo|4pdo]], [[4pd1|4pd1]], [[4tk1|4tk1]], [[4tk3|4tk3]], [[4tk4|4tk4]]</td></tr>
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">Gphn, Gph ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Buffalo rat])</td></tr>
<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=4tk2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4tk2 OCA], [http://pdbe.org/4tk2 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4tk2 RCSB], [http://www.ebi.ac.uk/pdbsum/4tk2 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4tk2 ProSAT]</span></td></tr>
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== Function ==
[[http://www.uniprot.org/uniprot/GEPH_RAT GEPH_RAT]] Microtubule-associated protein involved in membrane protein-cytoskeleton interactions. It is thought to anchor the inhibitory glycine receptor (GLYR) to subsynaptic microtubules (By similarity). Catalyzes two steps in the biosynthesis of the molybdenum cofactor. In the first step, molybdopterin is adenylated. Subsequently, molybdate is inserted into adenylated molybdopterin and AMP is released.<ref>PMID:8264797</ref> <ref>PMID:9990024</ref>  [[http://www.uniprot.org/uniprot/GBRA3_RAT GBRA3_RAT]] GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. 
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== Publication Abstract from PubMed ==
gamma-Aminobutyric acid type A and glycine receptors (GABAARs, GlyRs) are the major inhibitory neurotransmitter receptors and contribute to many synaptic functions, dysfunctions and human diseases. GABAARs are important drug targets regulated by direct interactions with the scaffolding protein gephyrin. Here we deduce the molecular basis of this interaction by chemical, biophysical and structural studies of the gephyrin-GABAAR alpha3 complex, revealing that the N-terminal region of the alpha3 peptide occupies the same binding site as the GlyR beta subunit, whereas the C-terminal moiety, which is conserved among all synaptic GABAAR alpha subunits, engages in unique interactions. Thermodynamic dissections of the gephyrin-receptor interactions identify two residues as primary determinants for gephyrin's subunit preference. This first structural evidence for the gephyrin-mediated synaptic accumulation of GABAARs offers a framework for future investigations into the regulation of inhibitory synaptic strength and for the development of mechanistically and therapeutically relevant compounds targeting the gephyrin-GABAAR interaction.

Molecular basis of the alternative recruitment of GABAA versus glycine receptors through gephyrin.,Maric HM, Kasaragod VB, Hausrat TJ, Kneussel M, Tretter V, Stromgaard K, Schindelin H Nat Commun. 2014 Dec 22;5:5767. doi: 10.1038/ncomms6767. PMID:25531214<ref>PMID:25531214</ref>

From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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==See Also==
*[[GABA receptor 3D structures|GABA receptor 3D structures]]
*[[Gephyrin|Gephyrin]]
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Buffalo rat]]
[[Category: Large Structures]]
[[Category: Kasaragod, V B]]
[[Category: Maric, H M]]
[[Category: Schindelin, H]]
[[Category: Biosynthetic protein]]
[[Category: Molybdenum co factor biosynthesis]]
[[Category: Neurotransmitter receptor anchoring]]
[[Category: Scaffolding protein]]
[[Category: Structural protein]]