Structural Integrity of the A147T Polymorph of Mammalian TSPO.

ABSTRACT: 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 important for the design of more potent diagnostic and therapeutic ligands of TSPO.

SUBMITTER: Jaremko M 

PROVIDER: S-EPMC5653209 | biostudies-literature | 2015 Jul

REPOSITORIES: biostudies-literature