期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 14, 期 24, 页码 8386-8395出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2006.09.002
关键词
sulfatase; inhibition; mechanism-based inhibition; proteomics
资金
- NIGMS NIH HHS [R37 GM044154-17, R37 GM044154] Funding Source: Medline
Several model mechanism-based inhibitors (MbIs) were designed and evaluated for their ability to inhibit sulfatases. The MbI motifs were based on simple aromatic sulfates, which are known to be commonly accepted substrates across this highly conserved enzyme class, so that they might be generally useful for sulfatase labeling studies. (Difluoro)methyl phenol sulfate analogs, constructed to release a reactive quinone methide trap, were not capable of irreversibly inactivating the sulfatase active site. On the other hand, the cyclic sulfamates (CySAs) demonstrated inhibition profiles consistent with an active site-directed mode of action. These molecules represent a novel scaffold for labeling sulfatases and for probing their catalytic mechanism. (c) 2006 Elsevier Ltd. All rights reserved.
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