Backbone and side-chain resonance assignment of the A147T polymorph of mouse TSPO in complex with a high-affinity radioligand
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The integral polytopic membrane protein TSPO is the target for numerous endogenous and synthetic ligands. However, the affinity of many ligands is influenced by a common polymorphism in TSPO, in which an alanine at position 147 is replaced by threonine, thereby complicating the use of several radioligands for clinical diagnosis. In contrast, the best-characterized TSPO ligand (R)-PK11195 binds with similar affinity to both variants of mitochondrial TSPO (wild-type and A147T variant). Here we report the 1H, 13C, 15N backbone and side-chain resonance assignment of the A147T polymorph of TSPO from Mus Musculus in complex with (R)-PK11195 in DPC detergent micelles. More than 90 % of all resonances were sequence-specifically assigned, demonstrating the ability to obtain high-quality spectral data for both the backbone and the side-chains of medically relevant integral membrane proteins.
KeywordsTSPO Polymorphism (R)-PK11195 NMR spectroscopy Membrane protein
1H, 13C, 15N resonance assignments of the A147T-mTSPO/PK11195 complex have been deposited at the BMRB data base (Accession Code: 25513). This work was partially supported by the DFG Collaborative Research Center 803, Project A11.
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No conflict declared.
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