2n02
Solution structure of the A147T variant of the mitochondrial translocator protein (tspo) in complex with pk11195
Structural highlights
FunctionTSPO_MOUSE Can bind protoporphyrin IX and may play a role in the transport of porphyrins and heme (By similarity). Was initially identified as peripheral-type benzodiazepine receptor; can also bind isoquinoline carboxamides. Promotes the transport of cholesterol across mitochondrial membranes and may play a role in lipid metabolism (PubMed:9832438, PubMed:24814875), but its precise physiological role is controversial. According to some reports, it is not required for steroid hormone biosynthesis (PubMed:24174323, PubMed:24936060).[1] [2] [3] [4] [5] Publication Abstract from PubMedLigands 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 of 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. Structural integrity of the A147T polymorph of mammalian TSPO.,Jaremko M, Jaremko L, Giller K, Becker S, Zweckstetter M Chembiochem. 2015 May 12. doi: 10.1002/cbic.201500217. PMID:25974690[6] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
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