2n02

From Proteopedia

(Difference between revisions)

Current revision

Solution structure of the A147T variant of the mitochondrial translocator protein (tspo) in complex with pk11195

Structural highlights

2n02 is a 1 chain structure with sequence from Mus musculus. Full experimental information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:	Solution NMR
Ligands:
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

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).^[1] ^[2] ^[3] ^[4] ^[5]

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^[6]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

↑ Morohaku K, Pelton SH, Daugherty DJ, Butler WR, Deng W, Selvaraj V. Translocator protein/peripheral benzodiazepine receptor is not required for steroid hormone biosynthesis. Endocrinology. 2014 Jan;155(1):89-97. PMID:24174323 doi:10.1210/en.2013-1556
↑ Taylor JM, Allen AM, Graham A. Targeting mitochondrial 18 kDa translocator protein (TSPO) regulates macrophage cholesterol efflux and lipid phenotype. Clin Sci (Lond). 2014 Nov;127(10):603-13. PMID:24814875 doi:10.1042/CS20140047
↑ Tu LN, Morohaku K, Manna PR, Pelton SH, Butler WR, Stocco DM, Selvaraj V. Peripheral benzodiazepine receptor/translocator protein global knock-out mice are viable with no effects on steroid hormone biosynthesis. J Biol Chem. 2014 Oct 3;289(40):27444-54. PMID:24936060 doi:10.1074/jbc.M114.578286
↑ Garnier M, Dimchev AB, Boujrad N, Price JM, Musto NA, Papadopoulos V. In vitro reconstitution of a functional peripheral-type benzodiazepine receptor from mouse Leydig tumor cells. Mol Pharmacol. 1994 Feb;45(2):201-11 PMID:8114671
↑ Li H, Papadopoulos V. Peripheral-type benzodiazepine receptor function in cholesterol transport. Identification of a putative cholesterol recognition/interaction amino acid sequence and consensus pattern. Endocrinology. 1998 Dec;139(12):4991-7. PMID:9832438 doi:10.1210/endo.139.12.6390
↑ Jaremko M, Jaremko L, Giller K, Becker S, Zweckstetter M. Structural integrity of the A147T polymorph of mammalian TSPO. Chembiochem. 2015 May 12. doi: 10.1002/cbic.201500217. PMID:25974690 doi:http://dx.doi.org/10.1002/cbic.201500217

1 Structural highlights
2 Function
3 Publication Abstract from PubMed
4 References

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/2n02"

@@ Line 4: / Line 4: @@
 == 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='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>
+</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>

2n02

From Proteopedia

Current revision

Solution structure of the A147T variant of the mitochondrial translocator protein (tspo) in complex with pk11195

Structural highlights

Function

Publication Abstract from PubMed

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

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