Article
Tricyclic heterocycles display diverse sensitivity to the A147T TSPO polymorphism.
European journal of medicinal chemistry - 1 Dec 2020
Sokias Renee, Werry Eryn L, Alison Cheng Hei Wun, Lloyd James H, Sohler Greta, Danon Jonathan J, Montgomery Andrew P, Du Jonathan J, Gao Quanqing, Hibbs David E, Ittner Lars M, Reekie Tristan A, Kassiou Michael
Abstract excerpt
The 18 kDa translocator protein (TSPO) is a target for the development of imaging agents to detect neuroinflammation. The clinical utility of second-generation TSPO ligands has been hindered by the presence of a polymorphism, rs6971, which causes a non-conservative substitution of alanine for threonine at amino acid residue 147 (TSPO A147T). Given the complex nature of TSPO binding, and the lack of...
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