Structural Integrity of the A147T Polymorph of Mammalian TSPO.
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ABSTRACT:
SUBMITTER: Jaremko M
PROVIDER: S-EPMC5653209 | biostudies-literature | 2015 Jul
REPOSITORIES: biostudies-literature
Publications
Structural Integrity of the A147T Polymorph of Mammalian TSPO.
Jaremko Mariusz M Jaremko Łukasz Ł Giller Karin K Becker Stefan S Zweckstetter Markus M
Chembiochem : a European journal of chemical biology 20150610 10
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 as the wild-type protein and thus binds PK11195 with comparable affinity. Our study is i ...[more]
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