2n02: Difference between revisions
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==Solution structure of the A147T variant of the mitochondrial translocator protein (tspo) in complex with pk11195== | |||
<StructureSection load='2n02' size='340' side='right'caption='[[2n02]]' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[2n02]] 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=2N02 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2N02 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=2n02 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2n02 OCA], [https://pdbe.org/2n02 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2n02 RCSB], [https://www.ebi.ac.uk/pdbsum/2n02 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2n02 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> | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
Ligands of the transmembrane protein TSPO are used for imaging of brain inflammation, but a common polymorphism in TSPO complicates their application to humans. Here we determined the three-dimensional structure and side chain dynamics of the A147T polymorph of mammalian TSPO in complex with the first-generation ligand PK11195. We show that A147T TSPO is able to retain the same structural and dynamic profile of the wild-type protein and thus binds PK11195 with comparable affinity. Our study is important for the design of more potent diagnostic and therapeutic ligands of TSPO. | |||
Structural integrity of the A147T polymorph of mammalian TSPO.,Jaremko M, Jaremko L, Giller K, Becker S, Zweckstetter M Chembiochem. 2015 May 12. doi: 10.1002/cbic.201500217. PMID:25974690<ref>PMID:25974690</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
[[Category: | </div> | ||
[[Category: Becker | <div class="pdbe-citations 2n02" style="background-color:#fffaf0;"></div> | ||
[[Category: | == References == | ||
[[Category: Jaremko | <references/> | ||
[[Category: | __TOC__ | ||
[[Category: | </StructureSection> | ||
[[Category: Large Structures]] | |||
[[Category: Mus musculus]] | |||
[[Category: Becker S]] | |||
[[Category: Giller K]] | |||
[[Category: Jaremko L]] | |||
[[Category: Jaremko M]] | |||
[[Category: Zweckstetter M]] | |||
Latest revision as of 06:12, 15 May 2024
Solution structure of the A147T variant of the mitochondrial translocator protein (tspo) in complex with pk11195
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