Synthesis and evaluation of geldanamycin-estradiol hybrids
Synthesis and evaluation of geldanamycin-estradiol hybrids
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DOI：
10.1016/s0960-894x(99)00185-7
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发表时间：
1999-05-03
影响因子：
2.7
通讯作者：
Danishefsky, SJ
中科院分区：
文献类型：
--
作者：
Kuduk, SD;Zheng, FF;Danishefsky, SJ
格尔德霉素（GDM）结合到热休克蛋白90分子伴侣蛋白，并导致几个重要的信号蛋白的降解。合成了一系列新的雌二醇-格尔德霉素杂合物，并评价了它们诱导雌激素受体（ER）选择性降解的能力。杂合化合物比母体化合物具有活性和更高的选择性，导致ER和HER 2降解，但不降解其他GDM靶标。(C)1999 Elsevier Science Ltd.保留所有权利。
Geldanamycin (GDM) binds to the Hsp90 chaperone protein and causes the degradation of several important signalling proteins. A series of novel estradiol-geldanamycin hybrids has been synthesized and evaluated for their ability to induce the selective degradation of the estrogen receptor (ER). The hybrid compounds are active and more selective than the parent causing degradation of ER and HER2, but not other GDM targets. (C) 1999 Elsevier Science Ltd. All rights reserved.