Structural highlights
Publication Abstract from PubMed
Ligands 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[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Jaremko M, Jaremko L, Giller K, Becker S, Zweckstetter M. Structural integrity of the A147T polymorph of mammalian TSPO. Chembiochem. 2015 May 12. doi: 10.1002/cbic.201500217. PMID:25974690 doi:http://dx.doi.org/10.1002/cbic.201500217
