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PDBsum entry 5olv
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Membrane protein
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PDB id
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5olv
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References listed in PDB file
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Key reference
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Title
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Towards high throughput gpcr crystallography: in meso soaking of adenosine a2areceptor crystals.
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Authors
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P.Rucktooa,
R.K.Y.Cheng,
E.Segala,
T.Geng,
J.C.Errey,
G.A.Brown,
R.M.Cooke,
F.H.Marshall,
A.S.Doré.
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Ref.
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Sci Rep, 2018,
8,
41.
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PubMed id
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Abstract
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Here we report an efficient method to generate multiple co-structures of the
A2AG 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).
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