期刊
CHEMISTRY-A EUROPEAN JOURNAL
卷 26, 期 50, 页码 11391-11403出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.202000584
关键词
drug discovery; fragment libraries; ligand design; NMR spectroscopy; X-ray crystallography
资金
- DTU Chemistry
- DK-OPENSCREEN from the Ministry of Higher Education and Science [5072-00019B]
- DTU
Fragment-based drug discovery (FBDD) has become an established approach for the generation of early lead candidates. However, despite its success and inherent advantages, hit-to-candidate progression for FBDD is not necessarily faster than that of traditional high-throughput screening. Thus, new technology-driven library design strategies have emerged as a means to facilitate more efficient fragment screening and/or subsequent fragment-to-hit chemistry. This minireview discusses such strategies, which cover the use of labeled fragments for NMR spectroscopy, X-ray crystallographic screening of specialized fragments, covalent linkage for mass spectrometry, dynamic combinatorial chemistry, and fragments optimized for easy elaboration.
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