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PDBsum entry 6tsh
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Sugar binding protein
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PDB id
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6tsh
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References listed in PDB file
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Key reference
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Title
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Fragment-Based drug discovery using cryo-Em.
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Authors
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M.Saur,
M.J.Hartshorn,
J.Dong,
J.Reeks,
G.Bunkoczi,
H.Jhoti,
P.A.Williams.
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Ref.
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Drug Discov Today, 2020,
25,
485-490.
[DOI no: ]
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PubMed id
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Abstract
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Recent advances in electron cryo-microscopy (cryo-EM) structure determination
have pushed the resolutions obtainable by the method into the range widely
considered to be of utility for drug discovery. Here, we review the use of
cryo-EM in fragment-based drug discovery (FBDD) based on in-house method
development. We demonstrate not only that cryo-EM can reveal details of the
molecular interactions between fragments and a protein, but also that the
current reproducibility, quality, and throughput are compatible with FBDD. We
exemplify this using the test system β-galactosidase (Bgal) and the oncology
target pyruvate kinase 2 (PKM2).
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