2MGY

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

2MGY の概要

• エントリーDOI: 10.2210/pdb2mgy/pdb
• NMR情報: BMRB: 19608
• 分子名称: Translocator protein, N-[(2R)-butan-2-yl]-1-(2-chlorophenyl)-N-methylisoquinoline-3-carboxamide (2 entities in total)
• 機能のキーワード: membrane protein, translocator protein (tspo), protein-ligand complex, mitochondrial membrane, pk11195, dpc micelles, peripheral benzodiazepine receptor, helical membrane channel protein
• 由来する生物種: Mus musculus (mouse)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 19151.54

構造登録者

Jaremko, M.,Jaremko, L.,Giller, K.,Becker, S.,Zweckstetter, M. (登録日: 2013-11-11, 公開日: 2014-04-02, 最終更新日: 2024-05-15)

主引用文献

Jaremko, 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

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

実験手法

SOLUTION NMR