View source for 2mgy


==Solution structure of the mitochondrial translocator protein (TSPO) in complex with its high-affinity ligand PK11195==
<StructureSection load='2mgy' size='340' side='right'caption='[[2mgy]]' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[2mgy]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2MGY OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2MGY FirstGlance]. <br>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Solution NMR</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=PKA:N-[(2R)-BUTAN-2-YL]-1-(2-CHLOROPHENYL)-N-METHYLISOQUINOLINE-3-CARBOXAMIDE'>PKA</scene></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2mgy FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2mgy OCA], [https://pdbe.org/2mgy PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2mgy RCSB], [https://www.ebi.ac.uk/pdbsum/2mgy PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2mgy ProSAT]</span></td></tr>
</table>
== Function ==
[https://www.uniprot.org/uniprot/TSPO_MOUSE TSPO_MOUSE] Can bind protoporphyrin IX and may play a role in the transport of porphyrins and heme (By similarity). Was initially identified as peripheral-type benzodiazepine receptor; can also bind isoquinoline carboxamides. Promotes the transport of cholesterol across mitochondrial membranes and may play a role in lipid metabolism (PubMed:9832438, PubMed:24814875), but its precise physiological role is controversial. According to some reports, it is not required for steroid hormone biosynthesis (PubMed:24174323, PubMed:24936060).<ref>PMID:24174323</ref> <ref>PMID:24814875</ref> <ref>PMID:24936060</ref> <ref>PMID:8114671</ref> <ref>PMID:9832438</ref> 
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== Publication Abstract from PubMed ==
The 18-kilodalton translocator protein TSPO is found in mitochondrial membranes and mediates the import of cholesterol and porphyrins into mitochondria. In line with the role of TSPO in mitochondrial function, TSPO ligands are used for a variety of diagnostic and therapeutic applications in animals and humans. We present the three-dimensional high-resolution structure of mammalian TSPO reconstituted in detergent micelles in complex with its high-affinity ligand PK11195. The TSPO-PK11195 structure is described by a tight bundle of five transmembrane alpha helices that form a hydrophobic pocket accepting PK11195. Ligand-induced stabilization of the structure of TSPO suggests a molecular mechanism for the stimulation of cholesterol transport into mitochondria.

Structure of the mitochondrial translocator protein in complex with a diagnostic ligand.,Jaremko L, Jaremko M, Giller K, Becker S, Zweckstetter M Science. 2014 Mar 21;343(6177):1363-6. doi: 10.1126/science.1248725. PMID:24653034<ref>PMID:24653034</ref>

From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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<div class="pdbe-citations 2mgy" style="background-color:#fffaf0;"></div>
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Large Structures]]
[[Category: Mus musculus]]
[[Category: Becker S]]
[[Category: Giller K]]
[[Category: Jaremko L]]
[[Category: Jaremko M]]
[[Category: Zweckstetter M]]