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- W4213060363 abstract "The G protein-coupled adenosine A2A receptor (A2A AR) is an important new (potential) drug target in immuno-oncology, and for neurodegenerative diseases. Preladenant and its derivatives belong to the most potent A2A AR antagonists displaying exceptional selectivity. While crystal structures of the human A2A AR have been solved, mostly using the A2A -StaR2 protein that bears 9 point mutations, co-crystallization with Preladenant derivatives has so far been elusive. We developed a new A2A AR construct harboring a single point mutation (S913.39 K) which renders it extremely thermostable. This allowed the co-crystallization of two novel Preladenant derivatives, the polyethylene glycol-conjugated (PEGylated) PSB-2113, and the fluorophore-labeled PSB-2115. The obtained crystal structures (2.25 Å and 2.6 Å resolution) provide explanations for the high potency and selectivity of Preladenant derivatives. They represent the first crystal structures of a GPCR in complex with PEG- and fluorophore-conjugated ligands. The applied strategy is predicted to be applicable to further class A GPCRs." @default.
- W4213060363 created "2022-02-24" @default.
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- W4213060363 date "2022-03-24" @default.
- W4213060363 modified "2023-10-16" @default.
- W4213060363 title "Single Stabilizing Point Mutation Enables High‐Resolution Co‐Crystal Structures of the Adenosine A <sub>2A</sub> Receptor with Preladenant Conjugates" @default.
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- W4213060363 doi "https://doi.org/10.1002/anie.202115545" @default.
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