Structure of the mammalian TSPO/PBR protein
| Autor: | Mariusz Jaremko, Stefan Becker, Garima Jaipuria, Markus Zweckstetter, Łukasz Jaremko |
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| Rok vydání: | 2015 |
| Předmět: |
Models
Molecular chemistry [Bacterial Proteins] metabolism [Bacterial Proteins] Endogeny Biochemistry Protein Structure Secondary 03 medical and health sciences Mice 0302 clinical medicine Bacterial Proteins Receptors GABA Translocator protein Animals Humans Binding site chemistry [Receptors GABA] Receptor 030304 developmental biology Mammals 0303 health sciences Binding Sites biology Bzrp protein mouse metabolism [Mammals] Ligand (biochemistry) Isoquinolines Transmembrane protein 3. Good health metabolism [Receptors GABA] ddc:540 PK 11195 biology.protein pharmacology [Isoquinolines] 030217 neurology & neurosurgery Synthetic ligands Function (biology) drug effects [Binding Sites] |
| Zdroj: | Biochemical Society Transactions Biochemical Society transactions 43(4), 566-571 (2015). doi:10.1042/BST20150029 |
| ISSN: | 1470-8752 |
| DOI: | 10.1042/BST20150029 |
| Popis: | The 3D structure of the 18-kDa transmembrane (TM) protein TSPO (translocator protein)/PBR (peripheral benzodiazepine receptor), which contains a binding site for benzodiazepines, is important to better understand its function and regulation by endogenous and synthetic ligands. We have recently determined the structure of mammalian TSPO/PBR in complex with the diagnostic ligand PK11195 [1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide; Jaremko et al. (2014) Science 343, 1363–1366], providing for the first time atomic-level insight into the conformation of this protein, which is up-regulated in various pathological conditions including Alzheimer's disease and Parkinson's disease. Here, we review the studies which have probed the structural properties of mammalian TSPO/PBR as well as the homologues bacterial tryptophan-rich sensory proteins (TspOs) over the years and provide detailed insight into the 3D structure of mouse TSPO (mTSPO)/PBR in complex with PK11195. |
| Databáze: | OpenAIRE |
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