期刊
DRUG DISCOVERY TODAY
卷 25, 期 3, 页码 485-490出版社
ELSEVIER SCI LTD
DOI: 10.1016/j.drudis.2019.12.006
关键词
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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 beta-galactosidase (Bgal) and the oncology target pyruvate kinase 2 (PKM2).
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