期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 59, 期 23, 页码 10794-10799出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.6b01117
关键词
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资金
- Swedish Research Council [621-2013-4749]
- University of Gothenburg
- COST Action [TD09056]
Photoaffinity labeling (PAL) was used to identify the binding site of chroman-4-one-based SIRT2-selective inhibitors. The photoactive diazirine 4, a potent SIRT2 inhibitor, was subjected to detailed photochemical characterization. In PAL experiments with SIRT2, a tryptic peptide originating from the covalent attachment of photo activated 4 was identified. The peptide covers both the active site of SIRT2 and the proposed binding site of chroman-4one-based inhibitors. A high-power LED was used as source for the monochromatic UV light enabling rapid photo activation.
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