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2MGY

Solution structure of the mitochondrial translocator protein (TSPO) in complex with its high-affinity ligand PK11195

Summary for 2MGY
Entry DOI10.2210/pdb2mgy/pdb
NMR InformationBMRB: 19608
DescriptorTranslocator protein, N-[(2R)-butan-2-yl]-1-(2-chlorophenyl)-N-methylisoquinoline-3-carboxamide (2 entities in total)
Functional Keywordsmembrane protein, translocator protein (tspo), protein-ligand complex, mitochondrial membrane, pk11195, dpc micelles, peripheral benzodiazepine receptor, helical membrane channel protein
Biological sourceMus musculus (mouse)
Total number of polymer chains1
Total formula weight19151.54
Authors
Jaremko, M.,Jaremko, L.,Giller, K.,Becker, S.,Zweckstetter, M. (deposition date: 2013-11-11, release date: 2014-04-02, Last modification date: 2024-05-15)
Primary citationJaremko, L.,Jaremko, M.,Giller, K.,Becker, S.,Zweckstetter, M.
Structure of the mitochondrial translocator protein in complex with a diagnostic ligand.
Science, 343:1363-1366, 2014
Cited by
PubMed Abstract: 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 α 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.
PubMed: 24653034
DOI: 10.1126/science.1248725
PDB entries with the same primary citation
Experimental method
SOLUTION NMR
Structure validation

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