期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 17, 期 2, 页码 320-325出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.10.101
关键词
natural products; biotin; crosslinking; secretion; golgi
资金
- NCI NIH HHS [R01 CA086079, CA 086079] Funding Source: Medline
- NIGMS NIH HHS [R01 GM046224, GM 53747, GM 46224, R01 GM053747] Funding Source: Medline
Inspired by the effect of norrisolide on the Golgi complex, we synthesized norrisolide probes that contain: the perhydroindane core of the parent natural product for Golgi localization, a crosslinking unit (aryl azide or epoxide) for covalent binding to the target, and a tag (biotin or iodine) for subsequent target purification. We found that biotin-containing probes 14, 20 and 24 induced inefficient Golgi vesiculation. However, the iodinated probe 25 induced extensive and irreversible Golgi fragmentation. This probe can be used for the isolation of the cellular target of norrisolide. (c) 2006 Elsevier Ltd. All rights reserved.
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