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Literature DB >> 25974690

Structural Integrity of the A147T Polymorph of Mammalian TSPO.

Mariusz Jaremko¹, Łukasz Jaremko^1,2, Karin Giller¹, Stefan Becker¹, Markus Zweckstetter^3,4,5.

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.

Entities: Chemical

Keywords: NMR spectroscopy; dynamics; membrane proteins; polymorphism; protein structures

Mesh：

Substances：

Year: 2015 PMID： 25974690 PMCID： PMC5653209 DOI： 10.1002/cbic.201500217

Source DB: PubMed Journal: Chembiochem ISSN： 1439-4227 Impact factor: 3.164

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