期刊
EXPERT OPINION ON THERAPEUTIC TARGETS
卷 8, 期 6, 页码 597-611出版社
TAYLOR & FRANCIS LTD
DOI: 10.1517/14728222.8.6.597
关键词
3-FABS; drug design; drug discovery; inter ligand nuclear Overhauser effect (ILOE); NMR; saturation transfer difference (STD); structure-activity relationships (SAR) by ILOE; SAR by NMR; structure-based iterative optimisations (SUBITO)
资金
- NIAID NIH HHS [AI058123, AI056385] Funding Source: Medline
In this review, the use of general NMR spectroscopy techniques to detect ligand binding and to monitor enzyme kinetics and inhibition, which appear particularly useful in hit identification and validation, is reiterated. Furthermore, the use of NMR-based strategies for lead optimisations that are based on either iterative derivatisations of an initial core structure or on linking fragments that occupy adjacent pockets in the target's binding site will also be described. Several recent examples will be reported and the use of these techniques in cases when the three dimensional structure of the target protein is known will be discussed.
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