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- W2782198436 abstract "Abstract Here we report an efficient method to generate multiple co-structures of the A 2A G protein-coupled receptor (GPCR) with small-molecules from a single preparation of a thermostabilised receptor crystallised in Lipidic Cubic Phase (LCP). Receptor crystallisation is achieved following purification using a low affinity “carrier” ligand (theophylline) and crystals are then soaked in solutions containing the desired (higher affinity) compounds. Complete datasets to high resolution can then be collected from single crystals and seven structures are reported here of which three are novel. The method significantly improves structural throughput for ligand screening using stabilised GPCRs, thereby actively driving Structure-Based Drug Discovery (SBDD)." @default.
- W2782198436 created "2018-01-12" @default.
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- W2782198436 date "2018-01-08" @default.
- W2782198436 modified "2023-10-11" @default.
- W2782198436 title "Towards high throughput GPCR crystallography: In Meso soaking of Adenosine A2A Receptor crystals" @default.
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- W2782198436 doi "https://doi.org/10.1038/s41598-017-18570-w" @default.
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