2N02
Solution structure of the A147T variant of the mitochondrial translocator protein (tspo) in complex with pk11195
Summary for 2N02
| Entry DOI | 10.2210/pdb2n02/pdb |
| Related | 2mgy |
| NMR Information | BMRB: 25513 |
| Descriptor | Translocator protein, N-[(2R)-butan-2-yl]-1-(2-chlorophenyl)-N-methylisoquinoline-3-carboxamide (2 entities in total) |
| Functional Keywords | membrane protein, translocator protein (tspo), protein-ligand complex, mitochondria, pk11195, peripheral benzodiazepine receptor, a147t |
| Biological source | Mus musculus (mouse) |
| Total number of polymer chains | 1 |
| Total formula weight | 19181.57 |
| Authors | Jaremko, M.,Jaremko, L.,Giller, K.,Becker, S.,Zweckstetter, M. (deposition date: 2015-03-04, release date: 2015-06-10, Last modification date: 2024-05-15) |
| Primary citation | Jaremko, M.,Jaremko, M.,Giller, K.,Becker, S.,Zweckstetter, M. Structural Integrity of the A147T Polymorph of Mammalian TSPO. Chembiochem, 16:1483-1489, 2015 Cited by PubMed Abstract: 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 as 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. PubMed: 25974690DOI: 10.1002/cbic.201500217 PDB entries with the same primary citation |
| Experimental method | SOLUTION NMR |
Structure validation
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