Chemical biology studies on norrisolide

Chemical biology studies on norrisolide
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DOI:
10.1016/j.bmc.2010.02.007
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发表时间:
2010-03-15
影响因子:
3.5
通讯作者:
Theodorakis, Emmanuel A.
Theodorakis, Emmanuel A.
中科院分区:
医学3区
文献类型:
--
作者:
Guizzunti, Gianni;Brady, Thomas P.;Theodorakis, Emmanuel A.

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研究了新型高尔基囊泡剂诺里索内酯(7)的细胞活性及其化学结构。这种天然产物诱导高尔基体膜的不可逆囊泡,并在高尔基体水平上阻断蛋白质的运输。7的高尔基定位和断裂效应取决于过氢茚核的存在,而断裂的不可逆性取决于7的乙酰基。研究表明,norrisolide的荧光衍生物能够定位于高尔基体,是研究高尔基体结构和功能的重要工具。(C) 2010 Elsevier Ltd.版权所有。
The cellular activity of norrisolide (7), a novel Golgi-vesiculating agent, was dissected as function of its chemical structure. This natural product induces irreversible vesiculation of the Golgi membranes and blocks protein transport at the level of the Golgi. The Golgi localization and fragmentation effects of 7 depend on the presence of the perhydroindane core, while the irreversibility of fragmentation depends on the acetyl group of 7. We show that fluorescent derivatives of norrisolide are able to localize to the Golgi apparatus and represent important tools for the study of the Golgi structure and function. (C) 2010 Elsevier Ltd. All rights reserved.