Synthesis and evaluation of geldanamycin-testosterone hybrids
Synthesis and evaluation of geldanamycin-testosterone hybrids
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DOI：
10.1016/s0960-894x(00)00208-0
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发表时间：
2000-06-05
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;Harris, CR;Danishefsky, SJ
格尔德霉素（GDM）与Hsp 90伴侣蛋白结合，导致几种重要信号蛋白的降解。已经合成了一系列GDM-睾酮连接的杂合体，并评估了其对前列腺癌细胞系的活性。具有最大活性的杂交体对含有雄激素受体的前列腺癌细胞表现出有效的和选择性的细胞毒性。(C)2000爱思唯尔科技有限公司版权所有。
Geldanamycin (GDM) binds to the Hsp90 chaperone protein resulting in the degradation of several important signaling proteins. A series of GDM-testosterone linked hybrids has been synthesized and evaluated for activity against prostate cancer cell lines. The hybrid with the greatest activity exhibits potent and selective cytotoxicity against prostate cancer cells containing the androgen receptor. (C) 2000 Elsevier Science Ltd. All rights reserved.