Structure of the mitochondrial translocator protein in complex with a diagnostic ligand

Lukasz Jaremko, Mariusz Jaremko, Karin Giller, Stefan Becker*, Markus Zweckstetter

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

164 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)1363-1366
Number of pages4
JournalScience
Volume343
Issue number6177
DOIs
StatePublished - Jan 1 2014

ASJC Scopus subject areas

  • Medicine(all)
  • General

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